| One pot synthesis and SAR of some novel 3-substituted 5,6-diphenyl-1,2,4-triazines as antifungal agents. | |
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MedLine Citation:
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PMID: 20005098 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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An improved protocol for the synthesis of a novel series of 1,2,4-triazines possessing 1,2,3-triazole and piperidine ring using 1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazole-4-carbohydrazide, benzil, ammonium acetate and ZrOCl(2).8H(2)O as a catalyst in ethanol-water has been presented. The yields obtained are in the range of 87-94%. All the synthesized compounds (4a-4l) are novel and were evaluated for their in vitro antifungal activity. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Based on activity data SAR for the series has been developed. Compound 4c from the series was equipotent to miconazole against Candida albicans (MIC-25), Aspergillus niger (MIC-12.5) and Cryptococcus neoformans (MIC-25). Compound 4d was equipotent with miconazole against all tested organisms except Cryptococcus neoformans. Also compound 4i was equipotent with miconazole against C. albicans, A. niger and Fusarium oxysporum. |
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Authors:
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Jaiprakash N Sangshetti; Devanand B Shinde |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2009-11-15 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 Jan |
Date Detail:
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Created Date: 2010-02-03 Completed Date: 2010-04-20 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 742-5 Citation Subset: IM |
Copyright Information:
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Copyright 2009 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004 (MS), India. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antifungal Agents
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chemical synthesis*,
chemistry,
pharmacology Catalysis Fluconazole / chemistry, pharmacology Miconazole / chemistry, pharmacology Microbial Sensitivity Tests Piperidines / chemistry Structure-Activity Relationship Triazines / chemical synthesis, chemistry*, pharmacology Zirconium / chemistry |
| Chemical | |
Reg. No./Substance:
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0/Antifungal Agents; 0/Piperidines; 0/Triazines; 110-89-4/piperidine; 22916-47-8/Miconazole; 290-38-0/1,2,4-triazine; 7440-67-7/Zirconium; 7699-43-6/zirconium oxychloride; 86386-73-4/Fluconazole |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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