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

Letters in Drug Design & Discovery

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

DOI: 10.2174/1570180811209050953

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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

Page: [953 - 957] Pages: 5

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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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