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Synthesis and antitubercular activity of 2-(substituted phenyl/benzyl-amino)-6-(4-chlorophenyl)-5-(methoxycarbonyl)-4-methyl-3,6-dihydropyrimidin-1-ium chlorides.

Authors
  • Narayanaswamy, Venugopala K
  • Nayak, Susanta K
  • Pillay, Melendhran
  • Prasanna, Renuka
  • Coovadia, Yacoob M
  • Odhav, Bharti
Type
Published Article
Journal
Chemical Biology & Drug Design
Publisher
Wiley (Blackwell Publishing)
Publication Date
Feb 01, 2013
Volume
81
Issue
2
Pages
219–227
Identifiers
DOI: 10.1111/cbdd.12065
PMID: 23150983
Source
Medline
License
Unknown

Abstract

A series of 2-(substituted phenyl/benzyl-amino)-6-(4-chlorophenyl)-5-(methoxycarbonyl)-4-methyl-3,6-dihydropyrimidin-1-ium chlorides 7-13 and 15 was synthesized in their hydrochloride salt form. The title compounds were characterized by FT-IR, NMR ((1)H and (13)C) and elemental analysis. They were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv, multidrug resistance tuberculosis and extensively drug resistance tuberculosis by agar diffusion method and tested for the cytotoxic action on peripheral blood mononuclear cells by MTT assay. Among all the tested compounds in the series, compounds 7 and 11 emerged as promising antitubercular agents at 16 μg/mL against multidrug resistance tuberculosis and over 64 μg/mL against extensively drug resistance tuberculosis. The conformational features and supramolecular assembly of the promising compounds 7 and 11 were determined by single crystal X-ray study.

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