Design, Synthesis of Pyridine Based Thiazolidine Derivatives and Investigation of Antimicrobial Activity Targeting Ergosterol Biosynthesis via In Vitro and In Silico Approaches

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Abstract
Pyridine and thiazolidine ring systems are unique heterocyclic rings since they are present in the structure of various drug/drug‐like molecules and reported in many studies for their distinct biological effects. It is of interest to pharmaceutical chemists because of their chemotherapeutic effect profiles such as antibacterial, antifungal, antiviral, and anticancer; briefly, their cytotoxic effects are very interesting. Because of these cytotoxic activities, in this project, we synthesized chalcone derivatives from the 5 th position of the thiazolidin‐4‐one and its linking pyridine by the hydrazone bridge. The antibacterial activities of the resulted compounds on different gram (+) and (−) bacteria and their antifungal activities tested against several invasive fungi. Due to significant fungistatic activity, the inhibitory activity on lanosterol demethylase (LDM, 5TZ1, CYP51A1) and aromatase (3EQM, CYP19A1) enzymes was evaluated, and in silico approaches were used to clarify and explain the binding modes, and then the structure activity relationship (SAR) was reported. Results of the study indicated that designed molecules were successfully obtained with important antifungal activity, and the mechanism of action was clarified.
Funding Information
  • Bilecik Şeyh Edebali Üniversitesi (2023‐01.BŞEÜ.12‐04)

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