Synthesis and Antitubercular Evaluation of Some Novel 1,2,3,6-tetrahydropyrimidine-5-carbonitrile
DOI:
https://doi.org/10.24297/jac.v9i3.1014Keywords:
1, 2, 3, 6-tetrahydropyrimidine-5-carbonitrile, ethyl N-ethoxycarbonylbenzimidate, cyanoacetanilide derivatives, antitubercular activity.Abstract
     In an attempt to find a new class of antitubercular agents, a series of 1,2,3,6-tetrahydropyrimidine-5-carbonitrile were prepared via the reaction of ethyl N-ethoxycarbonylbenzimidate 2a-b with cyanoacetanilide derivatives 1a-c. These compounds were screened for their antitubercular activity against M. tuberculosis. Several analogues, such as 2,6-dioxo-1-phenyl-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3a, 1-benzyl-2, 6-dioxo-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3c and 1-benzyl-2, 6-dioxo-4-phenyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3d exhibited a potent antitubercular activity with an MIC values ranging from 10-35 µg/ml. Structures of the newly synthesized compounds were established by spectral data and HRMS.
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