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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Antimycobacterial Agents: Synthesis and Biological Evaluation of Novel 4-(Substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3,4-tetrahydropyrimidine- 5-carboxamide Derivatives by Using One-pot Multicomponent Method

Author(s): Abdulrahman I. Almansour, Mohamed Ashraf Ali, Sadath Ali, Ang Chee Wei, Yeong Keng Yoon, Rusli Ismail, Tan Soo Choon, Suresh Pandian, Raju Suresh Kumar, Natarajan Arumugam and Hasnah Osman

Volume 9, Issue 10, 2012

Page: [953 - 957] Pages: 5

DOI: 10.2174/1570180811209050953

Price: $65

Abstract

The aim of this work was to synthesize a series of compounds to study their antimycobacterial potential. Eight compounds were found to be most active with minimum inhibitory concentration of less than 6μM and were more active than Isoniazid (INH) against Mycobacterium tuberculosis H37Rv (MTB). Compounds with electron withdrawing group substituted on the aryl ring were showing better activity. Among the fifteen newly synthesized compounds, compound 6- methyl-4-(4-nitrophenyl)-2-oxo-N-(pyridin-2-yl)-1,2,3,4tetrahydropyrimidine-5-carboxamide (B) was found to be the most active agent against MTB and INH resistant Mycobacterium tuberculosis (INHR-MTB) with minimum inhibitory concentration of <0.35 μM.

Keywords: Antimycobacterial, Biginelli, Dihydropyrimidine, One pot, Mycobacterium tuberculosis, multidrug-resistant TB, antituberculosis activity, nitroimidazoles, antitubercular activities


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