Quantitative Structure Activity Relationships Studies on Benzimidazole Derivatives as antibacterial agents against Escherichia coli
Abstract
In a continuing effort to develop novel Benzimidazole
endowed with better pharmacological profiles. A series of Benzimidazole
derivatives were designed on the basis of previously developed QSARs.
These drugs offer novel mechanisms of action and expanded spectrums
of activity over traditional treatment option. However, with these new
agents comes the need for increased awareness of the potential
interactions and toxicities associated with these drugs. The best models
for different antibacterial agents against Escherichia coli were first
validated by leave-one-out cross validation procedure. It was revealed
that topological, physicochemical and indicator parameters were found
to have overall significant correlationship with antibacterial activity
against Escherichia coli and these studies provide an insight to design
new molecules.
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References
D.H., Exploring QSAR,
Fundamentals and application in
chemistry and biology.,
American Chemical Society.,
Washington, DC, USA, (1995).
2. Hanch, C., Leo, A., Hoekman,
D.H., Exploring QSAR,
Hydrophobic, Electronic and
Steric Constants., American
Chemical Society., Washington,
DC, USA, (1995).
3. Goker, H., Alp, H., Synthesis
and potent antimicrobial activity
of some novel carboxamidines.,
Molecules., 10 (2000) 1377-
1386.
4. Melagraki, G., Afantitis.,
QSAR study on para substituted
aromatic sulfonamides as
carbonic anhydrase II inhibitors
using topological information
indices., Bioorg. Med. Chem.,
14 (2006) 1108-1114.
5. Delgado, D. N., In Wilson and
Gisvold’s Textbook of
Medicinal and Pharmaceutical
chemistry, 10th ed.; LippincottRavon: New York, (1998) 173.
6. Boiani, M., Imidazole and
benzimidazole derivatives as
chemotherapeutic agents., J.
Med. Chem., 5 (2005) 409-424.
7. Campbell, W.C.,
Benzimidazole: Veterinary uses.
Parasitol. Today., 6 (1990) 130-
133.
8. Ayhan-Kilcigil., G., Altanlar,
N., Synthesis and antifungal
properties of some
benzimidazole derivatives.,
Turk. J. Chem., 30 (2006) 223-
228.
9. Kus, C., Synthesis and
antioxidant properties of some
novel benzimidazole
derivatives on lipid
peroxidation in the rat liver.,
Arch. Pharm. Res., 27(2004)
156-163.
10. Zulu, I., Veitch, A.,
Albendazole chemotherapy
for AIDS related diarrhea in
zambia clinical,
parasitological and mucosal
response., Alim. Pharmacol.
Ther., 16 (2002) 595-601.
11. Kazimierczuk, Z, Upcroft,
J.A., Synthesis, antiprotozoal
and antibacterial activity of
nitro and halogeno substituted
benzimidazole derivative.,
Acta Biochim. Polon., 49-1
(2002) 185-195.
12. Didier, E.S., Stovall, M.E.,
Green, L.C., Brindley, P.J.,
Sestak, K., Didier, P.J.,
Epidemiology of
microsporidiosis sources and
modes of transmission., Vet.
Parasitol., 126 (2004) 145-
166.
13. Podunavac, S.O.,Quantitative
Structure activity relationships
to predict antibacterial effect
of some benzimidazole
derivatives., APTEFF. , 39
(2008) 181-191.14. Podunavac-Kuzmanovic, S.O.,
Cvetkovic, D.D., Biological
activity of zinc (II) and nickel
(II) complexes with some 2-
aminobenzimidazole
derivatives in microorganisms
of environmental relevance
synthesis., Centr. Eur. J.
Occupat. Environ. Med.,
10(2006)55-60.
15. Perisic,-Janjie, N.U.,
Podunavac-Kuzmanovic, S.O.,
Balaz, J.S., Vlaovic, D.,
Chromatographic behaviour
and lipophilicity of some
benzimidazole derivatives .,J.
Planar. Chromatogr.,
13(2000)123-129.
16. Podunavac-Kuzmanovic, S.O.,
Leovac, V.M., Perisic,-Janjie,
N.U., Rogan, J., Balaz, J.,
Complexes cobalt (II), Zinc
(II), Copper (II) with some
newly synthesized
benzimidazole derivatives and
their antibacterial activity., J.
Serb. Chem. Soc.,
64(1999)381-388.
17. Podunavac-Kuzmanovic, S.O.,
Markov, S.L., Antimicrobial
activity of Copper (II)
complexes with some
benzimidazole derivatives
against microorganism widely
distributed in the environment
., Centr. Eur. J. Occupat.
Environ. Med., 12(2006)61-
66.
18. Podunavac-Kuzmanovic, S.O.,
Cvetkovic, D.D., Antibacterial
evalution of some
benzimidazole derivatives and
their zinc (II) complexes., J.
Serb. Chem. Soc.,
75(2007)459-466.
19. Podunavac-Kuzmanovic, S.O.,
Markov, S.L., Barna, D.J.,
Relationship between the
lipophilicity and antifungal
activity of some
benzimidazole derivative., J.
Theor. Comp. Chem.,
6(2007)687-698.
20. Podunavac-Kuzmanovic, S.O.,
Cvetkovic, D.D., Anion effect
on antimicrobial activity of
metal complexes with
benzimidazole derivative.,
CICEQ., 13(2007)68-71.
21. Perisic,-Janjie, N.U.,
Podunavac-Kuzmanovic, S.O.,
RPTLC study of QSRR and
QSAR for some
benzimidazole derivatives., J.
Planar. Chromatography.,
21(2008)135-141.
22. Topliss, J.G., Edwards, R.P.,
Chance factors in studies of
quantitative structure activity
relationships., J. Med.
Chem.,22 (1979)1238-1244.
23. Snedecor, G.W., Cochran,
Statistical Methods ., Oxford
and IBH., New Delhi., India.,
(1967) 381.
24. Chaltterjee, S., Hadi, A.S.,
Price, B., Regression Analysis
by examples., wiley VCH.,
New York., USA.,2000.
25. Diudea, M.V., QSPR/QSAR
studies for molecular
descriptors., Nova Science .,
Huntington , New York.,
USA., 2000.
26. Golbraikh, A., Tropsha, J.,
Beware of q2., J. Mol. Graph.
Mod., 20(2002)269-276.
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