Abstract
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
Letters in Drug Design & Discovery
Title: Novel N-Substituted Thiazolidinones as Proton Pump Inhibitors and Potent Anti-Ulcer Agents: SAR Study
Volume: 6 Issue: 2
Author(s): S. Chandrappa, K. Vinaya, B. M. Srikanta, C.S. Ananda Kumar, N. R. Thimmegowda, S. R. Ranganatha, Shylaja M. Dharmesh and K. S. Rangappa
Affiliation:
Keywords: Thiazolidinone, 5-Formyl-2-methoxybenzoic acid, Alkyl halides, Anti-ulcer, Peptic ulcer, H+, K+- ATPase enzyme
Abstract: 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.
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Chandrappa S., Vinaya K., Srikanta M. B., Kumar Ananda C.S., Thimmegowda R. N., Ranganatha R. S., Dharmesh M. Shylaja and Rangappa S. K., Novel N-Substituted Thiazolidinones as Proton Pump Inhibitors and Potent Anti-Ulcer Agents: SAR Study, Letters in Drug Design & Discovery 2009; 6 (2) . https://dx.doi.org/10.2174/157018009787582697
DOI https://dx.doi.org/10.2174/157018009787582697 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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