| Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid. | |
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MedLine Citation:
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PMID: 20235688 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Tashfeen Akhtar; Shahid Hameed; Khalid M Khan; Ajmal Khan; Muhammad Iqbal Choudhary |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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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:
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Created Date: 2010-07-05 Completed Date: 2010-10-08 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101150203 Medline TA: J Enzyme Inhib Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 572-6 Citation Subset: IM |
Affiliation:
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Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Ulcer Agents Drug Design Enzyme Inhibitors / chemical synthesis, pharmacology Humans Inhibitory Concentration 50 Mandelic Acids / chemistry Oxadiazoles / chemical synthesis*, pharmacology Structure-Activity Relationship Triazoles / chemical synthesis*, pharmacology Urease / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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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 3.5.1.5/Urease |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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