Bicyclic [1,3,4] Thiadiazolo[3,2-α]Pyrimidine Analogues: Novel One-Pot Three-Component Synthesis, Antimicrobial, and Antioxidant Evaluation

被引：5

作者：

Bhadraiah, Umesha K. ^{[1
]}

Basavanna, Vrushabendra ^{[2
]}

Gurudatt, Doddahosuru M. ^{[3
]}

Shivalingappa, Rajendra Prasad ^{[4
]}

Lingegowda, Nagarakere S. ^{[2
]}

Ningaiah, Srikantamurthy ^{[2
]}

机构：

[1] Univ Mysore, Yuvarajas Coll, Dept Chem, Mysuru 570005, Karnataka, India

[2] Visvesvaraya Technol Univ, Vidyavardhaka Coll Engn, Dept Chem, Mysore 570002, Karnataka, India

[3] Univ Mysore, Dept Studies Organ Chem, Mysuru 570006, Karnataka, India

[4] Davangere Univ, PG Dept Chem, Davangere 577007, Karnataka, India

来源：

BIOINTERFACE RESEARCH IN APPLIED CHEMISTRY | 2021年 / 11卷 / 05期

关键词：

one-pot three-component synthesis; 1,3,4-thiadiazolo[3,2-a]pyrimidine; antibacterial activity; ANTITUMOR-ACTIVITY; DERIVATIVES; PYRIMIDINE; INHIBITORS; MECHANISM; SERIES;

D O I：

10.33263/BRIAC115.1292512936

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A novel one-pot three-component synthesis of 1-(7-methyl-2,5-diphenyl-5H-[1,3,4]thiadiazolo(3,2-alpha)pyrimidine-6-yl)ethanone (4a-i) derivatives via cyclo-condensation of substituted 2-amino-[1,3,4]-thiadiazole (1a-c), acetylacetone (2) and various aromatic aldehydes (3a-c) in the presence of p-toluene sulfonic acid (PTSA) in acetonitrile. Spectral data and elemental analysis have characterized the newly synthesized compounds. The new analogs were screened for their antibacterial and antifungal activities. The majority of the tested compounds displayed significant to moderate efficacy against most of the designated organisms. Among the tested compounds, 4b, 4e, and 4h showed noteworthy efficacy against selected microbes, and compounds 4c and 4i were found to be exceptionally efficient against selected fungal strains. Compound 4c, 4e, 4f, 4i were also designated as best antioxidants against NOx.

引用

页码：12925 / 12936

页数：12

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