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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Synthesis, Antimicrobial, Anticancer Evaluation and QSAR Studies of 3/4-Bromo Benzohydrazide Derivatives

Author(s): Pradeep Kumar, Balasubramanian Narasimhan, Kalavathy Ramasamy, Vasudevan Mani, Rakesh Kumar Mishra and Abu Bakar Abdul Majeed

Volume 15, Issue 11, 2015

Page: [1050 - 1064] Pages: 15

DOI: 10.2174/156802661511150408111252

Price: $65

Abstract

A series 3/4-bromo-N'-(substituted benzylidene/furan-2-ylmethylene/5-oxopentylidene/3- phenylallylidene)benzohydrazides (1-23) was synthesized and characterized by physicochemical and spectral means. The synthesized compounds were screened for their antimicrobial and anticancer potentials. Antimicrobial activity results indicated that compound 12 (pMICam = 1.67 μM/ml) was the most potent antimicrobial agent. The synthesized benzohydrazides were also having good anticancer potential and compound 22 (IC50 = 1.20 μM μM) was found to be the most potent anticancer agent which was more potent than standard drugs, tetrandrine (IC50 = 1.53) and 5- fluorouracil (IC50 = 4.6 μM). QSAR studies indicated that antimicrobial activity of synthesized compounds was best described by electronic parameter, total energy (Te) and topological parameters, valance zero order molecular connectivity index (0χv) and Wiener index (W).

Keywords: Anticancer activity, Antimicrobial activity, Benzohydrazides, Minimum bactericidal/fungicidal concentration, Minimum inhibitory concentration, QSAR studies.

Graphical Abstract


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