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

Autor: Janardhan Sridhara, Tejeswara Rao Allaka, Parsharamulu Rayam, Ramesh Ummanni, Jaya Shree Anireddy, Naveen Polkam, Sudha Sravanti Kotapalli, Narahari Sastry Garikapati
Rok vydání: 2016
Předmět:
Zdroj: Medicinal Chemistry Research. 25:977-993
ISSN: 1554-8120
1054-2523
DOI: 10.1007/s00044-016-1544-8
Popis: 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 Staphylococcusaureus 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.
Databáze: OpenAIRE
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