Design, synthesis and relational biological researches of novel acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds

VernacularTitle:新型乙酰基取代的磺胺叔胺巯基唑类和磺胺叔胺氨基唑类化合物的设计合成及相关抗微生物作用研究
Author: Dan-yang FENG ; Liu-xue ZHU ; Shi-ju YANG ; Rui YAN ; Hui-zhen ZHANG ; Ying WANG
Publication Type:Research Article
Keywords: sulfonamide; tertiary amine; azole; antibacterial; antifungal
From: Acta Pharmaceutica Sinica 2024;59(12):3315-3324
CountryChina
Language:Chinese
Abstract: As an important synthetic antibacterial drug, sulfonamides play an important role in the anti-infection field. Based on the research and development status of sulfonamides, this paper broke the classical structure of sulfanilamide, and designed and synthesized a series of acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds. The structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. The antimicrobial activity of synthesized compounds in vitro was tested. The antimicrobial activity of amino triazole compound 7a gave stronger activity against Pseudomonas aeruginosa than that of positive control drug norfloxacin, and its inhibitory activity against Staphylococcus aureus was close to that of norfloxacin. The interaction between compound 7a and calf thymus DNA was studied, and the docking experiment between this compound and DNA was also researched.