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

Chandrappa, S. and Vinaya, K. and Srikanta, B. M. and Ananda Kumar, C. S. and Prasanna, D. S. and Thimmegowda, N. R. and Shylaja M. Dharmesh and Rangappa, K. S. (2010) Inhibition of gastric H+, K+-ATPase by novel thiazolidinone derivatives. Journal of Sulfur Chemistry, 31 (3). pp. 189-196. ISSN 1741-6000

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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
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	LA manjunath user
Date Deposited:	29 Jul 2019 03:29
Last Modified:	09 May 2023 07:05
URI:	http://eprints.uni-mysore.ac.in/id/eprint/5986

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