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.res.in/id/eprint/10418 |
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