Azolyl pyrimidines-synthesis and antimicrobial activity / N. H. Basha, T. Rekha, V. Padmavathi [et al.] // AIP conference proceedings. - 2022. - Vol. 2390. - Ст. 020006 Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): CHEMICAL COMPOUNDS -- PHARMACEUTICALS -- ANTIMICROBIALS Аннотация: Amide unit is a privileged structural motif and is a constituent of proteins, natural products and pharmaceuticals. Amongst different heterocyclic scaffolds, azoles and pyrimidines are the prominent entities in pharmaceutical arena. The biopotency of these heterocycles have triggered to synthesize a variety of heteroaromatics – azoles linked with pyridines by amino acetamide group. The target molecules-azolylaminoacetamidopyrimidines were prepared by the reaction of methyl azolylglycinate with pyrimidinyl-2-amine in the presence of DMAP and triethylamine in dichloromethane under ultrasonication. The lead molecules were evaluated for antimicrobial activity. Nitro substituted 2-((4-(4-chlorofuran-2-yl)thiazole-2-yl)amino)-N-(4,6-diphenylpyrimidin-2-yl)acetamide (9c) displayed excellent antibacterial activity against B. subtilis greater than the standard drug Chloramphenicol. However, 9c and nitro substituted 2-((4-(4-chlorofuran-2-yl)-1H-imidazol-2-yl)amino)-N-(4,6-diphenylpyrimidin-2-yl)acetamide (10c) showed antifungal activity on A. niger greater than the standard drug Ketoconazole. |