Document Detail

Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.
MedLine Citation:
PMID:  20235688     Owner:  NLM     Status:  MEDLINE    
Some new structural type inhibitors of urease, i.e. 2,5-disubstituted-1,3,4-oxadiazoles (4a-e) and 4,5-disubstituted-1,2,4-triazole-3-thiones (5a-e) were synthesized in two steps from mandelic acid hydrazides (2a-e) and aryl isothiocyanates. The hydrazides in turn were synthesized from mandelic acid via esterification. Compounds 4a-e and 5a-e were evaluated against jack bean urease. Compounds 4d, 5b, and 5d were found to be more potent, with IC(50) values of 16.1 +/- 0.12 microM, 18.9 +/- 0.188 microM, and 16.7 +/- 0.178 microM, respectively, when compared to the standard (thiourea; IC(50) = 21.0 +/- 0.011 microM). These compounds may be subjected to further investigations for the development of antiulcer drugs.
Tashfeen Akhtar; Shahid Hameed; Khalid M Khan; Ajmal Khan; Muhammad Iqbal Choudhary
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of enzyme inhibition and medicinal chemistry     Volume:  25     ISSN:  1475-6374     ISO Abbreviation:  J Enzyme Inhib Med Chem     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-07-05     Completed Date:  2010-10-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101150203     Medline TA:  J Enzyme Inhib Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  572-6     Citation Subset:  IM    
Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
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MeSH Terms
Anti-Ulcer Agents
Drug Design
Enzyme Inhibitors / chemical synthesis,  pharmacology
Inhibitory Concentration 50
Mandelic Acids / chemistry
Oxadiazoles / chemical synthesis*,  pharmacology
Structure-Activity Relationship
Triazoles / chemical synthesis*,  pharmacology
Urease / antagonists & inhibitors*
Reg. No./Substance:
0/Anti-Ulcer Agents; 0/Enzyme Inhibitors; 0/Mandelic Acids; 0/Oxadiazoles; 0/Triazoles; 288-88-0/1,2,4-triazole; 90-64-2/mandelic acid; EC

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