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

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, Hasnah Osman

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

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 H37Rν (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.

Original languageEnglish
Pages (from-to)953-957
Number of pages5
JournalLetters in Drug Design and Discovery
Volume9
Issue number10
DOIs
Publication statusPublished - Dec 2012
Externally publishedYes

Keywords

  • Antimycobacterial
  • Biginelli
  • Dihydropyrimidine
  • One pot

Cite this