Synthesis of New Thiazole Derivatives Bearing Thiazolidin-4(5H)-One Structure and Evaluation of Their Antimicrobial Activity

Abstract

Antimicrobial resistance was first documented in a study published in the 1940s. Antimicrobial resistance is becoming a global health crisis. Because of this issue, new pharmaceuticals must be created. So, we set out to create some new thiazolidine-4-one derivatives and test their efficacy against bacteria. To get the final products, certain aryl aldehydes were reacted with 2-[(4,5-diphenylthiazol-2-yl)imino]thiazolidin-4-one. Antimicrobial activity of the produced compounds was tested against four species of Candida, five species of gram-negative bacteria, and four species of gram-positive bacteria. At least a 70% yield of the active compounds (4ah) was achieved. Antimicrobial activity was observed in every component. Compound 4f showed the most activity against C. glabrata (ATCC 24433) (MIC: 31.25 g/ml). The most effective compound against all bacterial species, but especially K. pneumoniae (NCTC 9633), was compound 4b (MIC: 62.5 g/ml). In contrast, E. coli (ATCC 25922) was shown to be most susceptible to compound 4c (MIC:31.25g/ml). All eight compounds (4a-4h) shown antibacterial activity against every kind of bacterium and fungal organism tested. The most effective compounds were found to be 4b (2,6-dichlorobenzylidene), 4c (2,6-dihydroxybenzylidene), 4f (1H-pyrrol-2- yl)methylene, 4g (4-triflouromethylbenzylidene), and 4h (2,3,4-trimethoxybenzylidene).

Keywords: Thiazole. Thiazolidin-4-one. Azoles. Antibacterial activity. Anticandidal activity