NDLI: Design, synthesis and biological activity evaluation of novel pefloxacin derivatives as potential antibacterial agents

Content Provider	Springer Nature Link
Author	Allaka, Tejeswara Rao Polkam, Naveen Rayam, Parsharamulu Sridhara, Janardhan Garikapati, Narahari Sastry Kotapalli, Sudha Sravanti Ummanni, Ramesh Anireddy, Jaya Shree
Copyright Year	2016
Abstract	A facile and efficient method for the synthesis of novel derivatives of pefloxacin hydrazone via condensation of various aldehydes and pefloxacin acid hydrazide using conventional as well as solvent-free microwave irradiation methods was reported. The biological activity of these compounds was screened using array of techniques and found to exhibit promising broad spectrum of antibacterial activity against Gram-positive and Gram-negative bacteria, moderate antimycobacterial activity against Mycobacterium smegmatis and moderate antifungal activity opposed to Aspergillus clavatus and Candida albicans. Cytotoxic assay of the title compounds was evaluated against human Pc-3 cancer cell lines, and interestingly, very good anticancer properties were shown by the compounds. To explore the binding mode of the compounds and understand the key active site residues with Staphylococcus aureus DNA gyrase, a molecular docking study has been performed. The results of the docking studies of the reported derivatives were quite promising and manifested strong non-bonded interactions with DNA Gyrase.
Starting Page	977
Ending Page	993
Page Count	17
File Format	PDF
ISSN	10542523
Journal	Medicinal Chemistry Research
Volume Number	25
Issue Number	5
e-ISSN	15548120
Language	English
Publisher	Springer US
Publisher Date	2016-03-03
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Antibacterial activity Anticancer activity Cytotoxic antibacterial DNA gyrase Docking studies Pefloxacin hydrazone Pharmacology/Toxicology Biochemistry Cell Biology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology, Toxicology and Pharmaceutics

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