Abstract
A series of N-alkyl benzimidazol piperazine fluoroquinolines with remarkable improvement in antimicrobial activity as compared to the moxifloxacin were synthesized and characterized by 1HNMR, 13C NMR, IR, Mass and elemental analysis. These derivatives were evaluated for their invitro activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae. The results showed that all the synthesized derivatives of novel fluoroquinolines possess antimicrobial activity. However, compound derivatives IV and V3 have antibacterial activities against Pseudomonas, Klebsiella and Staphylococcus epidermidis. Among all these derivatives, compound V3 exhibit potent inhibitory activity with MIC of 19 µg/mL.
Keywords: N-alkylbenzimidazolpiperazinefluoroquinolines, antimicrobial activity, MIC.
References
- Samuel, B. Medical Microbiology, 4th edition, chapter 7, 1996.
- Kenneth, T. Todar’s online text book of bacterialogy, Bacterial resistance to antibiotics, 2008, pg 1
- Rekha, B.; Alok, K.; Rajat, S.; Piyush, M. Asian J. Pharm. Clin.Res. 2009, 2, 164.
- Kapil, A.; Manish, A. Bioorg. Med. Chem. Lett. 2007, 17, 86.
- (a) Koga, H.; Itoh, A.; Murayama, S.; Suzue, S.; Irikura, T. J. Med. Chem. 1980, 23, 1358; (b) Hayakawa, I.; Hiramitsu, T.; Tanaka, Y. Chem. Pharm. Bull. 1984, 32, 4907; (c) Goueffon, Y.; Montay, G.; Roquot, F.; Pesson, M. C. R. Acad. Sci. Serie C 1981, 292, 37; (d) Hagen, S. E.; Domagala, J. M.; Heifetz, J. C. L.; Johnson, J. J. Med. Chem. 1991, 34, 1155; (e) Albini, A.; Monti, S. Chem. Soc. Rev. 2003, 32, 238; (f) Eric, M. S. J. Pharm. Educ. 2002, 66, 164.
- Muralidhar, N. V.; Subhashachandra, IN 2002MU00445, 2002; Chem. Abstr. 2005, 147:189078
- Rao, D. R.; Kankan, R. N. T.; Srinivas, P. L.; Ravikumar, P.; Manish, G.; Shashirekha, K. WO2008059223, 2008.
- Kuete, V.; Kamga, J.; Sandjo, L. P.; Ngameni, B.; Poumale, H. M.; Ambassa, P.; Ngadjui, B. T. BMC Complement. Altern. Med. 2011, 11, 6.
- Eloff, J. N. Planta Med. 1998, 64, 711.
- Mativandlela, S. P. N.; Lall, N.; Meyer, J. J. M. S. Afr. J. Bot. 2006, 72, 232.
- Tereschuk, M. L.; Riera, M. V. Q.; Castro, G. R.; Abdala, L. R. J. Ethnopharmacol.1997, 56, 227.
- Zgoda, J. R.; Porter, J. R.; Pharmaceut. Biol. 2001, 39, 221.
- Kuete, V.; Ngameni, B.; Fotso Simo, C. C.; Kengap Tankeu, R.; Tchaleu Ngadjui, B.; Meyer, J. J. M.; Lall, N.; Kuiate, J. R.; J. Ethnopharmacol. 2008, 120, 17.
- Cardoso, O.; Alves, A. F.; Leitao, R. M. Int. J. Infect. Dis. 2008, 12, 111.
- Carbonnelle, B.; Denis, F.; Marmonier, A.; Pinon, G.; Vague, R. Bactériologie médicale: Techniques usuelles. SIMEP, Paris; 1987
Corresponding Author
Prita S. Borkar
Department of Microbiology, NES Science College,
Nanded, Maharashtra, India-431605