Antimikobakteriyel Aktivite Göstermesi Beklenen Bazı 2,3-Disübstitüe-5-Metil-4-Tiyazolidinon Türevleri Üzerinde Çalışmalar

Abstract

Ekinci, A. S., Studies on Some 2,3-Disubstituted-5-Methyl-4-Thiazolidinone Derivatives Expected to Show Antimycobacterial Activity, Hacettepe University Graduate School of Health Sciences, MS Thesis in Pharmaceutical Chemistry, Ankara 2020. In this study, 11 compounds of 2-aryl-5-methyl-3-(phenylamino)thiazolidin-4-one (Compound 2a-k) derivative, one of which reported in the literature (Compound 2j), were synthesized and evaluated for the antimycobacterial activity. The chemical structures of synthesized compounds were proven by IR, 1H-/13C-NMR, mass spectroscopy methods, elemental analysis results and single-crystal X-ray crystallography. The antimycobacterial activities of the target compounds against the Mycobacterium tuberculosis H37Rv were investigated by the microplate alamar blue method, and the results were compared with reference compounds, isoniazid, rifampicin and ethambutol. Among the target compounds, 2-(4-ethylphenyl)-3-(phenylamino)-5-methylthiazolidin-4-one (Compound 2g) was found to be the most active derivative of the series with the minimum inhibitory concentration of 12.5 μg/mL of against M. tuberculosis. In the light of these findings, Compound 2g was considered the lead to reach more active compounds.