Inhibition of gastric H+, K+-ATPase by novel thiazolidinone derivatives

Article abstract of DOI:10.1080/17415991003702621

In a program to identify new anti-ulcer compounds, a series of novel substituted thiazolidinone derivatives 5(a-j) were synthesized and screened for their in vitro H⁺, K⁺-ATPase inhibitory activity. The synthesized compounds were characterized by nuclear magnetic resonance ( ¹H-NMR), liquid chromatography-mass spectrometry (LCMS) and fourier transform infrared (FTIR) analysis. We have briefly investigated the structure-activity relation (SAR) studies and reveal that the nature of position of the fluorine atom influences the anti-ulcer activity. Among the synthesized compounds 5b, 5c and 5e showed 4 and 10-fold higher H⁺, K ⁺-ATPase activity when compared with those of other derivatives 5a, 5f, 5g and 5j, respectively. H⁺, K⁺-ATPase activity of 5b, 5c and 5e were comparable with those of known H⁺, K ⁺-ATPase blocker lansoprazole which is a potential anti-ulcer drug.