| Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. | |
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MedLine Citation:
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PMID: 17569516 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Procedures were developed for the synthesis of 3-methyl-5-phenylethynyl[1,2,4]triazine (4), 6-methyl-3-phenylethynyl[1,2,4]triazine (5), and 5-methyl-3-phenylethynyl[1,2,4]triazine (6a) as analogues of 2-methyl-6-(phenylethynyl)pyridine (2). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. The most potent of the three analogues was 6a. Twenty additional analogues of 6a were synthesized and evaluated for mGluR5 antagonist efficacy. The most potent compounds were 3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine (6b), 5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine (6c), and 3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine (6d). |
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Authors:
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F Ivy Carroll; Sharadsrikar V Kotturi; Hernán A Navarro; S Wayne Mascarella; Brian P Gilmour; Forrest L Smith; Bichoy H Gabra; William L Dewey |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2007-06-15 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 50 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 2007 Jul |
Date Detail:
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Created Date: 2007-07-05 Completed Date: 2007-09-20 Revised Date: 2007-12-03 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 3388-91 Citation Subset: IM |
Affiliation:
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Center for Organic and Medicinal Chemistry, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA. fic@rti.org |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Drug Evaluation, Preclinical Magnetic Resonance Spectroscopy Pyridines / chemistry* Triazines / chemical synthesis*, pharmacology* |
| Grant Support | |
ID/Acronym/Agency:
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DA016472/DA/NIDA NIH HHS; DA05477/DA/NIDA NIH HHS; K05-DA00480/DA/NIDA NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/3-methyl-6-(phenylethynyl)pyridine; 0/Pyridines; 0/Triazines |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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