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. |
Bis(azolyl)sulfonamidoacetamides: Synthesis and bioassay / P. S. Sankar, K. N. Babu, V. N. Padmavathi [et al.] // AIP conference proceedings. - 2022. - Vol. 2390. - Ст. 020021 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ANTIMICROBIALS -- BIOASSAYS -- ANTIFUNGAL Аннотация: Azole derivatives are valuable precursors in pharmacological arena. In fact, oxazole, thiazole and imidazole containing scaffolds display a variety of biological activities such as antitumor,1 antibacterial,2 antiviral,3 antioxidant,4,5 anti-inflammatory6 and antifungal7 activities. Azoles are also prominant molecules in various biochemical and synthetic transformations. Based on the importance of these heteroaromatics and also our interest to link the heterocycle molecules with a variety of functional groups we have synthesized a new class of bis(azolyl)sulfonamide acetamides from azolylsulfonylamines and azolylchloroacetamides in the presence of DMAP under ultrasonication and studied their antimicrobial activity. The compounds chloro substituted bis(thiazoles) (6c) and chloro substituted imidazolyl thiazoles (7c) displayed excellent antibacterial activity against B. subtilis greater than the standard drug, Chloramphenicol. Whereas 7c also showed excellent antifungal activity on A. niger higher than the standard drug, Ketoconazole. |