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

Title: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

Volume: 9 Issue: 10

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

Affiliation:

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

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.

Cite this article as:

I. Almansour Abdulrahman, Ashraf Ali Mohamed, Ali Sadath, Chee Wei Ang, Keng Yoon Yeong, Ismail Rusli, Soo Choon Tan, Pandian Suresh, Suresh Kumar Raju, Arumugam Natarajan and Osman Hasnah, 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, Letters in Drug Design & Discovery 2012; 9 (10) . https://dx.doi.org/10.2174/1570180811209050953