Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Novel N-Substituted Thiazolidinones as Proton Pump Inhibitors and Potent Anti-Ulcer Agents: SAR Study

Author(s): S. Chandrappa, K. Vinaya, B. M. Srikanta, C.S. Ananda Kumar, N. R. Thimmegowda, S. R. Ranganatha, Shylaja M. Dharmesh, K. S. Rangappa.


A series of N-substituted thiazolidinone derivatives 5(a-j) was synthesized in good yield. All the compounds were screened for their in vitro H+, K+- ATPase inhibitory activity. The structures of the synthesized compounds were confirmed by the spectral data. Compounds 5d, 5e, 5f and 5c showed potential H+, K+- ATPase blocking activities, when compared to standard drug Lansoprazole. Structure-activity relationship studies, with various chemical groups, revealed that position and nature of the substitution on the N-thiazolidinones are crucial for H+, K+- ATPase inhibitory activity.

Keywords: Thiazolidinone, 5-Formyl-2-methoxybenzoic acid, Alkyl halides, Anti-ulcer, Peptic ulcer, H+, K+- ATPase enzyme

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Article Details

Year: 2009
Page: [101 - 106]
Pages: 6
DOI: 10.2174/157018009787582697
Price: $58