Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives.

Abstract:

:The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by molecular hybridization approach in which part C of the designed molecule was linked through amide and carbamate functionality that improves the physicochemical properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamide. All 52 compounds were evaluated for its antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound 11 g with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 μg/ml. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb.

journal_name

Eur J Med Chem

authors

Patel KN,Telvekar VN

doi

10.1016/j.ejmech.2014.01.024

subject

Has Abstract

pub_date

2014-03-21 00:00:00

pages

43-56

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00070-1

journal_volume

75

pub_type

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