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International Journal of Pharmacology

Year: 2013 | Volume: 9 | Issue: 7 | Page No.: 416-429
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Authors

Yun Fu

Yu Zhang

Sufeng Zhou

Youxun Liu

Jiangang Wang

Yali Wang

Chengbiao Lu

Changzheng Li

Keywords

Ciprofloxacin is one of fluoroquuinones widely used as antibiotics in clinical treatments. It has been shown that the carboxyl group on position 3 of ciprofloxacin is essential for antimicrobial activity, however, the amide form on this position and its corresponding biological effects have not been studied. To determine the structure-activity relationship, the ciprofloxacin hydrazide derivative was synthesized and its antimicrobial and antitumor mechanism was also evaluated preliminarily. Our results demonstrated that the substitution of -OH of carboxyl on position 3 of ciprofloxacin with a -NH-NH2 group could slightly alter the antimicrobial spectra, but not significantly. The studies of the hydrazide derivative on cell cycle arrest, mitochondrial membrane permeability, topoisomerase inhibition, pro-apoptotic gene regulation and molecular docking revealed that the minor structural modification on position 3 of ciprofloxacin did not result in changes in molecular targets compared to ciprofloxacin.
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How to cite this article

Yun Fu, Yu Zhang, Sufeng Zhou, Youxun Liu, Jiangang Wang, Yali Wang, Chengbiao Lu and Changzheng Li, 2013. Effects of Substitution of Carboxyl with Hydrazide Group on Position 3 of Ciprofloxacin on its Antimicrobial and Antitumor Activity. International Journal of Pharmacology, 9: 416-429.

DOI: 10.3923/ijp.2013.416.429

URL: https://scialert.net/abstract/?doi=ijp.2013.416.429

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