Synthesis and In Vitro Antimycobacterial Activity of Some New N-(5-Substituted Phenylthiazol-2-yl) Pyrimidine-5-Carboxamides

INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY(2023)

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摘要
A series of N-(5-substituted phenylthiazol-2-yl)pyrimidine-5-carboxamide derivatives (2a-j) was synthesized by the reaction of 5-substituted phenylthiazol-2-amines (1a-1j) and pyrimidine-5-carboxylic acid. Compounds 1a-1j were synthesized from acetophenones, thiourea, and iodine. The newly synthesized compounds 2a-j were characterized by IR, 1H NMR, 13C NMR, and mass spectral analysis and screened for their inhibitory effect against Mycobacterium tuberculosis H37Rv using the microplate Alamar blue assay method. Compounds 2i and 2j showed high antimycobacterial activity with MIC value of 6.25 & mu;g/mL, and compound 2h showed MIC value of 12.50 & mu;g/mL when compared with isoniazid (MIC value of 3.125 & mu;g/mL), pyrazinamide (MIC value 3.125 & mu;g/mL), and streptomycin (MIC value 6.25 & mu;g/mL) as reference drugs.
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关键词
Carboxamide derivatives, Aminothiazoles, Pyrimidine-5-carboxylic acid, Mycobacterium tuberculosis, Antimycobacterial activity
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