Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci.

, 2(1), 7-16

ISSN: 2231-2935
Review Article
www.ijrls.pharmascope.org

Medicinal significance of furan derivatives: A Review

Rumpa Banerjee, Kumar HKS, Mrityunjay Banerjee*
Department of Medicinal Chemistry, Institute of Pharmacy and Technology, Salipur, Cuttack, Odisha-754202, India
ABSTRACT
Furan is a planer five-member heterocyclic ring with 4C and 1O atom and in ring O is present in 1st positions. The
furan ring is a constituent of several important natural products, including furanoflavonoid, furanolactones, furanocoumarins and many natural terpenoids. Being a non polar aromatic compound and presence of the ether oxygen which adds polarity as well as the potential for hydrogen bonding, it improves pharmacokinetic characteristics
of lead molecules and thus used as a remedy to optimize solubility and bioavailability parameters of proposed
poorly soluble lead molecules. Furan derivatives have occupied a unique place in the field of medicinal chemistry.
The incorporation of the furan nucleus is an important synthetic strategy in drug discovery. The high therapeutic
properties of the furan related drugs have encouraged the medicinal chemists to synthesize a large number of
novel chemotherapeutic agents. drugs have broadened scope in remedying various dispositions in clinical medicines. Numerous methods for the synthesis of furans and also their various structure reactions offer enormous
scope in the field of medicinal chemistry. This articles aims to review the work reported, their chemistry and biological activities of furans during past years.
Keywords: Anti anxiolytic; anti bacterial; anti cholinergic; anti fungal; anti glaucoma; anti histamine; anti neoplastic; anti viral.
INTRODUCTION
Medicinal chemistry is the discipline which determines
the influence of chemical structure on biological activity and the practice of medicinal chemistry involves the
organic synthesis of new compound based largely on
the modification of structure and identifying their biological activity. Medicinal chemistry concerns with the
discovery, development, interpretation and the identification of mechanism of action of biologically active
compounds at the molecular level. Every drug has specific target in the body. These targets or receptors are
believed to be associated with disease and disorder.
The newly discovered compounds interact with these
receptors to show their potentiality to treat the disease or disorder. The high therapeutic properties of
the furan related drugs have encouraged the medicinal
chemists to synthesize a large number of novel chemotherapeutic agents which can act on various targets or
receptors in the body like they act as MAO inhibitors,
kappa opioid receptor agonist, sigma receptor agonist,
GABA receptor agonist, COX-2 inhibitor, Beta blockers,
opioid receptor agonist, muscarinic receptor agonist,
-adrenergic blockers, calcium channel blockers etc.
Furan drugs have broadened scope in remedying vari* Corresponding Author
Email: mrityunjaybanerjeepharmacy@gmail.com
Contact: +91-9437919100
Received on: 14.01.2012
Revised on: 22.02.2012
Accepted on: 22.03.2012

ous dispositions in clinical medicines. Medicinal properties of Furan include anticancer, antidepressant, antianxiolytic, analgesic, anti-inflammatory, muscle relaxant, antihypertensive, antiarrhythmic, antimicrobial
like antibacterial or antifungal or antiviral, antiaging
agents, anti-ulcer, antihistaminic, anticholinergic, antiparkinsonism, antidiuretic, and inhibition of sickle cell
formation. Infectious microbial disease causes worldwide problem, because microbes have resisted prophylaxis or therapy longer than any other form of life. In
recent decades, problems of multidrug-resistant microorganisms have reached an alarming level in many
countries around the world. Resistance of antimicrobial agents such as -lactam antibiotics, macrolides, quinolones and vancomycin etc. and different
species of bacteria causes increased important global
problem (Shingalapur RV et al., 2009).
Structure and pharmacological activities
Furans are well known heterocyclic compounds which
are common and have important feature of a variety of
medicinal agents. Furan is a 5-membered planar ring,
which is soluble in most organic solvents. It is the most
reactive compound of the 5-membered heterocyclic
compounds. It is a nonpolar compound. The electrophilic substitution reactions of furan take place preferably in 2-position. On account of its high reactivity very
mild reagents are required as compared to other compounds. Compounds containing the furan ring are generally excellent solvents. Some are miscible with both
water and with hexane. Presence of the ether oxygen
adds polarity as well as potential for hydrogen bond-

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Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci., 2(1), 7-16

ing. Compound containing the furan or tetra hydrofuran ring are biologically active and are present in a
number of pharmaceutical products. Furfurylamine is
an intermediate in the diuretic, furosemide. Tetra hydro furfurylamine may also have pharmaceutical applications. 5-(Dimethyl amine methyl) furfuryl alcohol is
an intermediate in the preparation of ranitidine, which
is used for treating ulcers. 2-Acetylfuran, prepared
from acetic anhydride and furan is an intermediate in
the synthesis of cefuroxime, a penicillin derivative. 2Furoic acid is prepared by the oxidation of furfural.
Both furoic acid and furoyl chloride are used as pharmaceutical intermediates. 2-Tetrahydrofuroic acid also
finds applications.
On the basis of various literature surveys furan derivatives shows various pharmacological activities
Antidepressant activity.
Antianxiolytic activity.
Anti inflammatory activity and analgesic activity.
Muscle relaxant drugs.
Antihypertensive drugs
Antiarrhythmic drugs.

Siramesine (Lu 28-179) is a sigma receptor agonist,

selective for the 2 subtype (Soby KK et al., 2002). In
animal studies, siramesine has been shown to produce
anxiolytic (Sanchez C et al., 1997) and antidepressant
(Sanchez C and Papp M, 2000) effects.

1'- {4- [1- (4- fluorophenyl) -1H- indol -3- yl] butyl} 3H- spiro [2- benzofuran -1, 4'- piperidine]
Antianxiolytic activity
Vilazodone (De Paulis T, 2007) (marketed as Viibryd) is
by Clinical Data for the treatment of major depressive
disorder. By 2009 two phase III clinical an antidepressant developed trials with positive results had been
completed. Vilazodone was approved by the FDA for
use in the United States to treat major depressive disorder in 10mg, 20mg, and 40mg doses on January the
21st, 2011

Antimicrobial activity.
Antiglaucoma activity.
Steroidal activity.
Anti-ulcer activity.
Antidiuretic activity.

5- (4- [4- (5- cyano -1H- indol -3- yl) butyl] piperazin 1- yl) benzofuran -2- carboxamide

Anorectic activity.
Inhibition of sickle cell formation.

NS-2664 is an anxiolytic drug (Mirza NR and Nielsen E,

2006).

Antiageing activity.
Antiparkinsonism activity
Antihistaminic and anticholinergic activity
Antineoplastic activity
Insectiside activity.

5- furan -3- yl -1- (3- imidazol -1- yl- phenyl) -1Hbenzoimidazole

Antidepressant activity
Geiparvarin is a coumarin derivative found in the
leaves of the Australian Willow (Geijera parviflora) (Lahey FN and Macleod JK, 1967). It is a monoamine oxidase inhibitor (Carotti A et al., 2002) and has antitumor
properties (Baraldi PG et al., 1989; Valenti P et
al.,1997; Viola G et al., 2004).

7- {[(2E) -3- (5, 5- dimethyl 4 oxo - 4, 5

dihydrofuran 2 yl) but -2- en -1- yl] oxy} -2Hchromen -2- one
8

BHFF is a compound used as a positive allosteric modulator at the GABAB receptor. It has anxiolytic effects
in animal studies, and good oral bioavailability (Malherbe P et al., 2008).

5, 7- bis (1, 1 - dimethylethyl) - 3 hydroxyl 3 (tri

fluoro methyl) -2 (3H) benzofuranone

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Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci., 2(1), 7-16

Analgesic and anti-inflammatory activity

2-Ethoxy methyl Salvinorin B is a semi-synthetic analogue of the natural product salvinorin A and has increased affinity and intrinsic activity at the -opioid
receptor (Munro TA et al., 2008).

17- (2- (furan -2- yl) ethyl) -3- hydroxymorphinan

Muscle relaxant activity

(2S, 4aR, 6aR, 7R, 9S, 10aS, 10bR) - 9 - (ethoxy methoxy) 2 - (3 - furanyl) dodecahydro -6a, 10b dimethyl - 4, 10 dioxo - 2H naphtha - [2, 1- c] pyran 7 carboxylic acid methyl ester

Dantrolene is a muscle relaxant that acts by abolishing

excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor and decreasing
intracellular calcium concentration (Krause T et al.,
2004).

Firocoxib is a non-steroidal anti-inflammatory drug of

the COX-2 inhibitor (coxib) class.
1- {[5- (4-nitrophenyl) -2- furyl] methylidene amino}
imidazolidine - 2, 4 - dione
Antihypertensive activity
Ancarolol is an antihypertensive agent and acts as a
beta blocker.
3- (Cyclopropyl methoxy) 5, 5 dimethyl 4 - (4
methyl sulfonyl phenyl) furan -2- one
Rofecoxib is a nonsteroidal anti-inflammatory drug
(NSAID) used to treat osteoarthritis, acute pain conditions, and dysmenorrhoea and has now been withdrawn over safety concerns about increased risk of
heart attack and stroke (Padi S and Kulkarni S, 2004).
Rofecoxib is a selective COX-2 inhibitor.

4- (4- methylsulfonylphenyl) -3- phenyl -5H- furan -2one

Mirfentanil is a fentanyl derivative with strong selectivity for the opioid receptor (France CP et al., 1991;
Carr DJ et al., 1996).

N- [2- [3- (tert-butyl amino) -2- hydroxy-propoxy]

phenyl] furan -2- carboxamide
Prazosin is a sympatholytic drug used to treat high
blood pressure (hypertension) (Shen and Howar,
2008). It belongs to the class of alpha-adrenergic
blockers.

2- [4- (2-furoyl) piperazin-1-yl] -6,7- dimethoxy quinazolin -4- amine

Terazosin (Tripathy KD, 2009a) is a selective alpha 1
antagonist used for treatment of symptoms of an enlarged prostate (BPH). It also acts to lower the blood
pressure.

N- [1- (2-phenylethyl) piperidin-4-yl]-N-pyrazin-2-yl-2furamide

Ro4-1539 (Furethyl nor levorphanol) is an opioid analgesic drug from the morphinan series. It acts as a potent -opioid agonist (Hellerbach J et al., 1966).

6, 7- dimethoxy -2- [4- (tetrahydrofuran -2-yl carbonyl) piperazin -1- yl] quinazolin -4- amine

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Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci., 2(1), 7-16

Antiarrhythmic activity

Antimicrobial activity

Azimilid (Braunwald E et al., 2001) is a class antiarrhythmic drug (used to control abnormal heart
rhythms).

Ceftiofur is an antibiotic of the cephalosporin type

(third generation) (Donaldson SC et al., 2006).

1- ({(E)- [5- (4- chloro phenyl) furan -2- yl] methylidene} amino) -3- [4- (4-methylpiperazin-1-yl) butyl]
imidazolidine -2,4- dione
Amiodarone is a class III anti arrhythmic agent. It is
used in the treatment of angina pectoris (P Cote et al.,
1979; Singh BN and Vaughan Williams EM, 1970). The
injection should not be given to neonates, because the
benzyl alcohol it contains may cause the fatal "gasping
syndrome".

(2-{4-[(2-butyl-1-benzofuran-3-yl) carbonyl] -2, 6- diiodophenoxy} ethyl) diethyl amine

Dronedarone (Dale KM and White CM, 2007) is a drug
used mainly for the indication of cardiac arrhythmias
(irregular heartbeat). It was approved by the FDA on
July 2, 2009. It is used for the treatment of atrial fibrillation and atrial flutter.

(6R, 7R) -7- [[(2Z) -2- (2-Amino-1, 3- thiazol -4- yl) -2methoxy imino acetyl] amino] -3-(furan-2- carbonyl
sulfanyl methyl) -8- oxo -5- thia -1- azabicyclo [4.2.0]
oct -2- ene -2-carboxylic acid
Cefuroxime is a second-generation cephalosporin antibiotic (Pichichero ME, 2006). It can cross the bloodbrain-barrier.

(6R, 7R) -3- {[(aminocarbonyl) oxy] methyl} -7- {[(2E) 2- (2-furyl) -2- (methoxyimino) acetyl] amino} -8- oxo5- thia -1- azabicyclo [4.2.0] oct -2- ene -2- carboxylic
acid
Nalfurafine is a -opioid receptor agonist marketed as
a treatment for uremic pruritus in people undergoing
hemodialysis. As of January 2010, it is also being investigated for the treatment of pruritus in patients with
chronic liver disease (Kevin KC et al., 2011).

N- (2- Butyl -3- (p- (3- (dibutylamino) propoxy) benzoyl) - 5- benzofuranyl) methane sulfonamide
Lanatoside C (Trease GE and Evans WC, 2005) is a cardiac glycoside, which can be used by the intravenous
route. Its main indications are rapid responde atrial
fibrilation and paroxistic supraventricular tachycardia.

(3, 5, 12) -3- {*-D- glucopyranosyl- (14)- 3-Oacetyl- 2,6-dideoxy- -D-ribo- hexopyranosyl- (14)2,6-dideoxy- -D- ribo- hexopyranosyl- (14)- 2,6dideoxy- -D- ribo- hexopyranosyl]oxy}- 12,14dihydroxycard- 20(22)- enolide

10

(2E) -N- *(5, 6) -17- (cyclopropylmethyl) -3, 14dihydroxy -4,5- epoxy morphinan - 6- yl] -3- (3-furyl)N-methylacrylamide
Roseophilin is an antibiotic isolated from Streptomyces
griscovirides (Furstner A, 2003).

15- [5- (3- Chloro -1H- pyrrol -2- yl) -3- methoxy furan 2- yl] -13- isopropyl -2- aza-tricyclo [10.2.1.13, 14]
hexadeca-1(15), 2-triene

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Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci., 2(1), 7-16

Santonin is a drug which was widely used in the past as

an anthelminthic. Large doses, however, produce toxic
effects, aphasia, muscular tremors and epileptiform
convulsions, and the disturbances of vision may go on
to total blindness (Modern Drug 1995).

Nifuroxazide is an oral nitrofuran antibiotic, patented

since 1966 and used to treat colitis and diarrhea in
humans and non-humans (USPTO).

4- Hydroxy -N'- [(5- nitrofuran -2-yl) methylene] benzohydrazide

(3S, 3aS, 5aS, 9bS) -3, 5a, 9 trimethyl - 3a, 5, 5a, 9b
tetra hydro naphtha [1, 2 -b] furan-2, 8 (3H, 4H) - dione

Nifurquinazol (NF-1088) is an antibacterial agent of the

nitrofuran class (Chapman and Hall 1996). It was never
marketed.

Diloxanide furoate is an anti-protozoal drug used in the

treatment of Entamoeba histolytica (Fernandes H et
al., 2009) and some other protozoal infections.

4-[(dichloroacetyl) (methyl) amino] phenyl furan-2carboxylate

Fumoxicillin is an antibiotic. This antibacterial agent is a
prodrug of amoxicillin which increases bioavailability
(Daniel Lednicer 1990).

(2S, 5R, 6R) -6- [[(R)- [(2- Furanyl methylene) amino]

(4-hydroxyphenyl) acetyl] amino] -3,3- dimethyl -7oxo -4- thia -1- azabicyclo [3.2.0] heptanes -2- carboxylic acid
Furazolidone is an antibacterial. It is used to treat diarrhoea and enteritis caused by bacteria or protozoan
infections (H. Parham and B Aibaghi Esfahani, 2008).
Itis also used for Giardiasis.

3- {[(5- nitro -2- furyl) methylene] amino} -1,3oxazolidin -2- one

Nifuratel (R N Gruneberg and A Leakey, 1976) is a drug
used in gynecology. It is a local antiprotozoal and antifungal agent that may also be given orally.

5-[(methylthio) methyl] -3- {[(1E)- (5-nitro-2-furyl)

methylene] amino} -1,3- oxazolidin -2- one

2,2'- {[2-(5- nitrofuran -2- yl) quinazolin -4- yl] imino}

diethanol
Nifurtoinol is a nitrofuran-derivative antibiotic used in
the treatment of urinary tract infections. It is also
known as "hydroxymethylnitrofurantoin" (Stricker BH
et al., 1988).

3- (hydroxyl methyl) -1- {[(1E)- (5- nitro -2-furyl) methylene] amino} imidazolidine -2,4- dione
Nitrofurantoin (KD Tripathy 2009 b) is an antibiotic. It is
usually used in treating urinary tract infection.

(E) -1- [(5- nitro -2- furyl) methylidene amino] imidazolidine -2, 4- dione
Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease
(Coura JR and De Castro SL, 2002) and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is in a Phase II clinical trial for the treatment of
pediatric neuroblastoma and medulloblastoma.

(RS) -3- methyl -N- [(1E)-(5- nitro -2-furyl) methylene]

thiomorpholin -4- amine 1,1- dioxide
Nitrofurazone (KD Tripathy 2009 c) is a bactericidal
compound is used as an antibiotic.

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5-nitro-2-furaldehyde semicarbazone
Antigluaucoma activity
Pilocarpine (KD Tripathy 2009 d) is a parasympathomimetic alkaloid obtained from the leaves of the genus
Pilocarpus. It is a non-selective muscarinic receptor
agonist. Pilocarpine has been used in the treatment of
chronic open-angle glaucoma and acute angle-closure
glaucoma for over 100 years. Pilocarpine is often used
as an antidote for scopolamine, atropine, and hyoscyamine poisoning.

2- ({2- [({5- [(dimethylamino) methyl] furan -2-yl} methyl) sulfanyl] ethyl} amino) -5- [(6- methylpyridin -3yl) methyl] pyrimidin -4(3H)- one
Niperotidine is a histamine antagonist selective for the
H2 subtype. It was trialled as a treatment for excessive
gastric acidity (Palasciano G et al., 1990), but withdrawn after human trials showed liver damage (Gasbarrini G et al., 1997).

(3S, 4R) - 3- ethyl - 4- ((1- methyl -1H- imidazol -5- yl)

methyl) dihydrofuran- 2(3H)-one
Steroidal activity
Fluticasone furoate is a synthetic corticosteroid derived
from fluticasone, used for the treatment of allergic
rhinitis. It can be administered by a nasal spray (Bruni
FM et al., 2009).

(Z) -N- (1, 3- benzodioxol -5- ylmethyl) -N'- {2[({5[(dimethylamino) methyl] -2- furyl} methyl) thio]
ethyl} -2- nitroethylene -1,1-diamine
Ranitidine (KD Tripathy 2009 e) is a histamine H2receptor antagonist that inhibits stomach acid production. It is used in treatment of peptic ulcer disease and
gastroesophageal reflux disease (GERD).

N- (2- [(5- (dimethyl amino methyl) furan -2-yl) methyl

thio] ethyl) -N- methyl -2- nitroethene -1, 1- diamine
(6, 11, 16, 17) -6, 9- difluoro -17- {[(fluoromethyl) thio] carbonyl} -11- hydroxy-16-methyl-3oxoandrosta -1, 4- dien -17- yl 2- furancarboxylate

Anorectic activity
Furfenorex is a stimulant used as an appetite suppressant. It produces abuse.

Mometasone furoate is a glucocorticoid steroid used

topically to reduce inflammation of the skin or in the
airways. It is used in the treatment of inflammatory
skin disorders (Tan RA and Corren J, 2008).
(RS)-N-(furan-2-ylmethyl)-N-methyl-1-phenylpropan2-amine

(11, 16) -9, 21- dichloro -11- hydroxyl -16- methyl-3,

20- dioxopregna -1,4- dien -17- yl 2-furoate

YM-348 is an indazole derivative drug which acts as a

potent and selective 5-HT2C receptor agonist, It has
thermogenic and anorectic effects in animal studies,
making it potentially useful for the treatment of obesity (Hayashi A et al., 2004; Smith BM et al., 2006; Nilsson BM 2006; Wacker DA and Miller KJ 2008).

Antiulcer activity
Lupitidine is an H2 receptor antagonist described as an
antiulcer agent (Lam BL, Pridgen LN, 1982).
(2S) -1- (7- ethyl -1H- furo [2,3-g] indazol -1- yl) propan -2- amine
12

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Diuretic activity
Furosemide is a loop diuretic used in the treatment of
hypertension, congestive heart failure and edema. It is
also sometimes used in the management of severe
hypercalcemia in combination with adequate rehydration (Rossi S 2004).

4- chloro -2- (furan -2- yl methyl amino) -5-sulfamoyl

benzoic acid
Inhibition of formation of sickle cell
Hydroxymethyl furfural inhibits the formation of sickled
cells in the blood (Abdulmalik et al., 2005).

2- furan -2- yl -7- (2- [4- (2- methoxyethoxy) phenyl]

piperazine -1- ylethyl)-7,9a- dihydro -5H- pyrazolo
[4,3-e] [1,2,4] triazolo [1,5-c] pyrimidin -5- amine
SCH-442,416 is a highly selective adenosine A2a subtype
receptor antagonist used in the treatment of depression (El Yacoubi M et al., 2003), Parkinson's disease
[58]
(Matsuya T et al., 2007), and catalepsy (Mihara T et
al., 2008).

5-(hydroxymethyl) -2- furaldehyde

Antiageing activity
Kinetin is a kind of cytokinin, a class of plant hormone
that promotes cell division. Since 1994, kinetin has
been thoroughly tested for its powerful anti-aging effects in human skin cells.

2- (2- f uryl) -7- [3- (4- methoxyphenyl) propyl] -7Hpyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin -5amine
Antineoplastic activity

N6- furfuryl adenine

Lapatinib used in the treatment of breast cancer and

other solid tumours (Burris HA 2004). It is a dual tyrosine kinase inhibitor which interrupts the HER2 growth
receptor pathway (Higa GM & Abraham J 2007). Like
many small molecule tyrosine kinase inhibitors, lapatinib is regarded as well tolerated.

Antiparkinsonian activity
ZM-241,385 is useful for the treatment of Alzheimer's
disease (Dalligna OP et al., 2004) and Parkinson's disease (Goembiowska K et al., 2004).

N- [3- chloro -4- [(3- fluoro phenyl) methoxy] phenyl] 6- [5- [(2- methyl sulfonyl ethyl amino) methyl] -2furyl] quinazolin-4-amine
CONCLUSION
(2- (7- amino -2- (furan -2- yl) - [1, 2, 4] triazolo [1, 5-a]
[1, 3, 5] triazin -5- yl amino) ethyl) phenol
Preladenant(SCH-420,814) acts as a potent and selective antagonist at the adenosine A2A receptor. It is being researched as a potential treatment for Parkinson's
disease (Hodgson RA et al., 2009).

The reviewed furan moiety has shown a wide spectrum

of biological activities. The various substituted furan
are having significant antimicrobial activity. Significant
antiviral and anti asthmatic activity is displayed by
some effective substituted furan derivative which presently leading drug in the market in entire. Some modified furans are found to be effective as anti-

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hypertensive, antiulcer, whereas some of the derivatives of furan are found to show the anti-asthmatic,
anti-viral action. Recently it was proven that some of
the important marketed furan nucleous containing
drug having different biological or pharmacological
activity were discussed in above text. The furan nucleous based pharmaceutical are rapidly becoming very
important class of therapeutic agents and are likely to
replace many existing organic based pharmaceuticals
in the very near future. The furan based pharmaceuticals will be produced on a large scale by modern drug
discovery company by different research development
processes and will become available commercially for
therapeutic use. With the key benefits including favorable time to market and high rate of success in clinical
trial compared with traditional pharmaceuticals due to
diverse biological action with less toxicity, so in future
therapeutic furan drug will play a pivotal role in the
treatment of different diseases. The biological profiles
of this new generation of furan represent much
progress with regard to the older compounds.
REFERENCES
Abdulmalik O, Safo MK, Chen Q, Yang J, Brugnara C,
Ohene-Frempong K, Abraham DJ, Asakura T. 5hydroxymethyl-2-furfural modifies intracellular sickle
haemoglobin and inhibits sickling of red blood cells.
British journal of haematology. 2005; 128 (4): 552
61.
Baraldi PG, Guarneri M, Manfredini S, Simoni D, Balzarini J, De Clercq E. Synthesis and cytostatic activity of
geiparvarin analogues. J Med Chem 1989; 32 (2):
2848.
Boissier JR, Dumont C, Ratouis R, Moisy D. Pharmacologic study of an anorexigenic agent: furfenorex.
Archives internationales de pharmacodynamie et de
therapie 1967; 167 (1): 15062.
Braunwald E, Zipes P, Libby P. Heart Disease A Textbook of Cardiovascular Medicine 6th edition. W.B.
Saunders Company. 2001; 717-736.
Bruni FM, De Luca G, Venturoli V, Boner AL. Intranasal
corticosteroids and adrenal suppression. Neuroimmunomodulation. 2009; 16 (5): 35362.
Burris HA. Dual kinase inhibition in the treatment of
breast cancer: initial experience with the EGFR/ErbB2 inhibitor lapatinib. Oncologist 2004; 9 (3): 105.
Carotti A, Carrieri A, Chimichi S. Natural and synthetic
geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies. Bioorg. Med. Chem.
Lett. 12 (24): 35515.
Carr DJ, Brockunier LL, Scott M, Bagley JR, France CP.
Mirfentanil antagonizes morphine-induced suppression of splenic NK activity in mice. Immunopharmacology. 1996; 34(1):9-16.

14

Kevin KC, Liua Subas M, Sakyab, Christopher J.

ODonnellb, Andrew C. Flickb, Jin Li. Synthetic approaches to the 2009 new drugs, Bioorganic & Medicinal Chemistry. 2011; 19(3): 11361154.
Coura JR, De Castro SL. A critical review of Chagas disease chemotherapy. Mem Inst Oswaldo Cruz. 2002;
97(1): 324
Dale KM, White CM. Dronedarone: an amiodarone
analog for the treatment of atrial fibrillation and
atrial flutter. Ann Pharmacother. 2007; 41 (4): 599
605.
Dalligna OP, Porcincula LO, Souza DO, Cunha RA, Lara
DR, Dall'lgna OP. Neuroprotection by caffeine and
adenosine A2A receptor blockade of beta-amyloid
neurotoxicity. British journal of pharmacology. 2003;
138 (7): 12079.
De Paulis T. Drug evaluation: Vilazodone--a combined
SSRI and 5-HT1A partial agonist for the treatment of
depression. IDrugs : the Investigational Drugs Journal. 2007; 10 (3): 193201.
Chapman, Hall. Dictionary of organic compounds. London. 6th ed. 1996.
Donaldson SC, Straley BA, Hegde NV, Sawant AA, DebRoy C, Jayarao BM. Molecular epidemiology of ceftiofur-resistant Escherichia coli isolates from dairy
calves. Appl. Environ. Microbiol. 2006; 72 (6): 3940
8.
H. Parham, B. Aibaghi Esfahani. Determination of Furazolidone in Urine by Square-Wave Voltammetric Method. J. Iran. Chem. Soc. 2008; 5(3): 453-457.
El Yacoubi M, Costentin J, Vaugeois JM. Adenosine A2A
receptors and depression. Neurology. 2003 Dec 9; 61
11 (6): 82-7.
Fernandes H, D'Souza CR, Swethadri GK, Naik CN.
Ameboma of the colon with amebic liver abscess
mimicking metastatic colon cancer. Indian J Pathol
Microbiol 2009; 52 (2): 22830.
France CP, Winger G, Medzihradsky F, Seggel MR, Rice
KC, Woods JH. Mirfentanil: pharmacological profile
of a novel fentanyl derivative with opioid and nonopioid effects. Journal of Pharmacology and Experimental Therapeutics. 1991; 258(2): 502-10.
Furstner A. Chemistry and biology of roseophilin and
the prodigiosin alkaloids: A survey of the last 2500
years. Angew. Chem., Int. Ed. 2003; 42: 3582-3603.
Gasbarrini G, Gentiloni N, Febbraro S, Gasbarrini A, Di
Campli C, Cesana M, Miglio F, Miglioli M, Ghinelli F,
D'Ambrosi A, Amoroso P, Pacini F, Salvadori G. Acute
liver injury related to the use of niperotidine. Journal
of Hepatology. 1997; 27(3):583-6. PMID 9314138
Goembiowska K, Dziubina A. Striatal adenosine A(2A)
receptor blockade increases extracellular dopamine
release following l-DOPA administration in intact and

JK Welfare & Pharmascope Foundation | International Journal of Review in Life Sciences

Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci., 2(1), 7-16

dopamine-denervated
2004; 47 (3): 41426.

rats.

Neuropharmacology.

Hayashi A, Sonoda R, Kimura Y, Takasu T, Suzuki M,

Sasamata M, Miyata K. Antiobesity effect of YM348,
a novel 5-HT2C receptor agonist, in Zucker rats. Brain
research. 2004; 1011 (2): 2217.
Hellerbach J, Schnider O, Besendorf H, Pellmont B. Synthetic Analgesics. Part IIA. Morphinans. Pergamon
Press, 1966.
Higa GM, Abraham J. Lapatinib in the treatment of
breast cancer (log in required). Expert Review of Anticancer Therapy (Future Drugs). 2007; 7 (9): 1183
92.
Hodgson RA, Bertorelli R, Varty GB, Lachowicz JE, Forlani A, Fredduzzi S, Cohen-Williams ME, Higgins GA,
Impagnatiello F, Nicolussi E, Parra LE, Foster C, Zhai
Y, Neustadt BR, Stamford AW, Parker EM, Reggiani A,
Hunter JC. Characterization of the Potent and Highly
Selective A2A Receptor Antagonists Preladenant and
SCH 412348 in Rodent Models of Movement Disorders and Depression. The Journal of Pharmacology
and Experimental Therapeutics. 2009; 330 (1): 294
303.
KD Tripathy, Essentials of medicaL pharmacology, Jaypee Brothers Medical Publishers (P) Limited, New
Delhi. 6th Ed. 2009: (a)134; (b)735; (c) 862; (d) 97-98;
(e) 630.
Krause T, Gerbershagen MU, Fiege M, Weisshorn R,
Wappler F. Dantrolene a review of its pharmacology, therapeutic use and new developments. Anaesthesia. 2004; 59 (4): 36473
Lahey FN, Macleod JK. The coumarins of Geijera parviflora Lindl. Aust J Chem. 1967; 20 (9): 194355.
Lam BL, Pridgen LN. U.S. Patent 1982; 4 (352): 933.
Malherbe P, Masciadri R, Norcross RD, Knoflach F,
Kratzeisen C, Zenner MT, Kolb Y, Marcuz A. Characterization
of
(R,S)-5,7-di-tert-butyl-3-hydroxy-3trifluoromethyl-3H-benzofuran-2-one as a positive
allosteric modulator of GABAB receptors. British
journal of pharmacology. 2008; 154 (4): 797811.
Matsuya T, Takuma K, Sato K, Asai M, Murakami Y,
Miyoshi S, Noda A, Nagai T, Mizoguchi H, Nishimura
S, Yamada K. Synergistic effects of adenosine A2A
antagonist and L-DOPA on rotational behaviors in 6hydroxydopamine - induced hemi - Parkinsonian
mouse model. Journal of Pharmacological Sciences.
2007; 103 (3): 329-32.
Mihara T, Noda A, Arai H, Mihara K, Iwashita A, Murakami Y, Matsuya T, Miyoshi S, Nishimura S, Matsuoka
N. Brain adenosine A2A receptor occupancy by a
novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: relationship to anticataleptic effect.
Journal of Nuclear Medicine. 2008; 49(7): 1183-8.

Mirza NR, Nielsen E. Do subtype-selective gammaaminobutyric acid A receptor modulators have a reduced propensity to induce physical dependence in
mice? Journal of Pharmacology and Experimental
Therapeutics. 2006; 316(3): 21.
Modern Drug Encyclopedia and Therapeutic Index,
Sixth Edition, Drug Publications Inc., New York, 1955.
Munro TA, Duncan KK, Xu W, Wang Y, Liu-Chen LY,
Carlezon WA, Cohen BM, Bguin C. Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. Bioorganic &
Medicinal Chemistry. 2008; 16 (3): 127986.
Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor
agonists as potential antiobesity agents. Journal of
medicinal chemistry. 2006; 49 (14): 402334..
Padi S, Kulkarni S. Differential effects of naproxen and
rofecoxib on the development of hypersensitivity following nerve injury in rats. Pharmacology, biochemistry and behavior. 2004; 79 (2): 349358.
Palasciano G, Maggi V, Portincasa P. The effect of the
H2-antagonist niperotidine on intragastric acidity in
healthy subjects undergoing 24-hour pH-monitoring.
Italian Journal of Gastroenterology. 1990; 22(5): 2914. PMID 1983712
Pichichero ME. Cephalosporins can be prescribed safely for penicillin-allergic patients. The Journal of family practice. 2006; 55 (2): 10612
R N Gruneberg, A Leakey. Treatment of candidal urinary tract infection with nifuratel. British Medical
Journal. 1976; 2: 908-910
R. V. Shingalapur, K. M. Hosamani, R.S. Keri. European
Journal of Medicinal Chemistry. 2009; 44: 42444248
Rossi S. Australian Medicines Handbook (5th ed.). Adelaide, S.A.: Australian Medicines Handbook Pty Ltd.
2004.
Sanchez C, Arnt J, Costall B, Kelly ME, Meier E, Naylor
RJ, Perregaard J. The selective sigma2-ligand Lu 28179 has potent anxiolytic-like effects in rodents.
Journal of Pharmacology and Experimental Therapeutics. 1997; 283(3): 1323-32.
Sanchez C, Papp M. The selective sigma2 ligand Lu 28179 has an antidepressant-like profile in the rat
chronic mild stress model of depression. Behavioural
Pharmacology. 2000; 11(2): 117-24
Shen, Howard. Illustrated Pharmacology Memory
Cards: Phar Mnemonics. Minireview. 2008; 13.
Singh BN, Vaughan Williams EM. The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br.
J. Pharmacol. 1970; 39 (4): 65767.
Smith BM, Thomsen WJ, Grottick AJ. The potential use
of selective 5-HT2C agonists in treating obesity. Ex-

JK Welfare & Pharmascope Foundation | International Journal of Review in Life Sciences

15

Mrityunjay Banerjee et al., (2012) Int. J. Rev. Life. Sci., 2(1), 7-16

pert opinion on investigational drugs. 2006; 15 (3):

25766.
Soby KK, Mikkelsen JD, Meier E, Thomsen C. Lu 28-179
labels a sigma(2)-site in rat and human brain. Neuropharmacology. 2002; 43(1):95-100.
Stricker BH, Blok AP, Claas FH, Van Parys GE, Desmet
VJ. Hepatic injury associated with the use of nitrofurans: a clinicopathological study of 52 reported cases. Hepatology. 1988.
P Cote, MG Bourassa, J Delaye, A Janin, R Froment, P
David. Effects of amiodarone on cardiac and coronary hemodynamics and on myocardial metabolism
in patients with coronary artery disease. Circulation
1979; 59: 1165-1172.
Daniel Lednicer, Lester A Mitscher, Gunda I Georg. The
organic chemistry of drug synthesis. A WileyInterscience Publication, John Wiley & Sons, Inc. New
York. 1990; 4: 5.
Tan RA, Corren J. Mometasone furoate in the management of asthma: a review. Ther Clin Risk Manag
2008; 4 (6): 12018. PMID 19337427
Valenti P, Rampa A, Recanatini M. Synthesis, cytotoxicity and SAR of simple geiparvarin analogues. Anticancer Drug Des. 1997; 12 (6): 44351.
Viola G, Vedaldi D, dall'Acqua F. Synthesis, cytotoxicity,
and apoptosis induction in human tumor cells by
geiparvarin analogues. Chem Biodivers 2004; 1(9)
Wacker DA, Miller KJ. Agonists of the serotonin 5-HT2C
receptor: preclinical and clinical progression in multiple diseases. Current opinion in drug discovery &
development. 2008;
Trease GE, Evans WC. Pharmacognosy. 15th ed. Edinburgh: W.B. Saunders. Elsevier, A division of Reed Elsevier India Private Limited, New Delhi, India. 2005;
310.

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