Antiproliferative-antimicrobial properties and structural analysis of newly synthesized Schiff bases derived from some 1,3,4-thiadiazole compounds

摘要: Abstract The 1,3,4-thiadiazole core has been mainly used as a pharmacological scaffold in medicinal chemistry. A series of Schiff bases derived from 5-substituted-1,3,4-thiadiazole-2-amine were designed and synthesized to investigate their biological activities. Structures compounds clarified with FTIR, 1H NMR elemental analysis. Due the importance this pharmacology, all these newly tested for different properties at same time. Compound 3A ((E)-N-(2,5-dimethoxybenzylidene)-5-(4-methoxyquinolin-2-yl)-1,3,4-thiadiazol-2-amine) compound 4A ((E)-N-(2,5-dimethoxybenzylidene)-5-(3-methylbenzofuran-2-yl)-1,3,4-thiadiazol-2-amine) possessed high DNA protective ability against oxidative Fenton mixture. 1A ((E)-N-(2,5-dimethoxybenzylidene)-5-(benzo[b]thiophen-2-yl)-1,3,4-thiadiazol-2-amine) 2B ((E)-2-((5-(1H-indol-2-yl)-1,3,4-thiadiazol-2-ylimino)methyl)-6-methoxyphenol) showed strong antimicrobial activity S. epidermidis. most effective was detected which exhibited cytotoxicity on both PC-3 MDA-MB-231 cancer cell lines. IC50 calculated 370.7 μM 505.1 μM PC-3 cells, respectively. Molecular docking studies also performed examine understanding mechanism behind anti-cancer anti-bacterial properties. For further study, potential utilization chemotherapy drugs establish more efficient therapy strategy minimum cells.