Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Research Abstract Details 

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Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Abstract Text:

F Ivy Carroll,Sharadsrikar V Kotturi, Navarro,S Wayne Mascarella,Brian P Gilmour,Forrest L Smith,Bichoy H Gabra,William L Dewey,

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).

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Publishing Authors By Initials

FI Carroll,SV Kotturi,HA Navarro,SW Mascarella,BP Gilmour,FL Smith,BH Gabra,WL Dewey,

For similar heterocyclic compounds: heterocyclic compounds, 1-ring: triazines research abstracts see: heterocyclic compounds: heterocyclic compounds, 1-ring: triazines research

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Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 3388-91

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 15

MONTH: 06

YEAR: 2007

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9716531

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Keywords Mesh Terms:

KEYWORDS: Triazines

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. Information

Substance Name: Triazines

Registry Number: 0

Grant and Affiliation Information for Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.

AFFILIATION: Center for Organic and Medicinal Chemistry, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA. fic@rti.org

Country: United States

AGENCY: United States NIDA

GRANT: K05-DA00480

ACRONYM: DA

MEDLINETA: J Med Chem

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