Synthesis and biological evaluation of quinolines, thiazolo[3,2-a]pyrimidines, thiadiazolo[3,2-a]pyrimidines and triazolo[3,4-b][1,3,4]thiadiazepines as antimicrobial agents

摘要

Series of quinolines, thiazolo[3,2-a]pyrimidines, thiadiazolo[3,2-a]pyrimidines and triazolo[3,4-b][1,3,4]thiadiazepines were synthesized by the reaction of amino compound, aromatic aldehyde and malononitrile/ethyl cyanoacetate, using 2-[5-(4-methoxyphenyl)-4H-1,2,4-triazol-3-ylthio]acetic acid as an organocatalyst in water-ethanol mixture. Synthesized compounds were evaluated for in vitro antibacterial and antifungal activities against three fungal and five bacterial strains. Some of them exhibited good activity in comparison with the standard fluconazole and streptomycin such as compound 16h has shown best antifungal activity with MIC value of 60 A mu g/mL against A. niger and 12g exhibited best antibacterial activity with MIC value of 50 A mu g/mL against E. coli.