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

Chandrappa, S. and Vinaya, K. and Srikanta, B. M. and Ananda Kumar, C. S. (2010) Inhibition of gastric H+, K+-ATPase by novel thiazolidinone derivatives. Journal of Sulfur Chemistry, 31 (3). pp. 189-196.

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Abstract

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.

Item Type: Article
Uncontrolled Keywords: thiazolidinone; 5-(3-chlorophenyl)-furfural; alkyl halides; anti-ulcer; H+, K+-ATPase enzyme
Subjects: 600 Technology > 01 Medical sciences > 15 Pharmacology
Divisions: Dept. of Biochemistry
Depositing User: Food Sci. & Technol. Information Services
Date Deposited: 05 Aug 2011 11:30
Last Modified: 26 Apr 2012 06:19
URI: http://ir.cftri.com/id/eprint/10418

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