28735-24-2Relevant articles and documents
Synthesis and pharmacological evaluation of phenylethynyl[1,2,4] methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine
Carroll, F. Ivy,Kotturi, Sharadsrikar V.,Navarro, Hernán A.,Mascarella, S. Wayne,Gilmour, Brian P.,Smith, Forrest L.,Gabra, Bichoy H.,Dewey, William L.
, p. 3388 - 3391 (2007)
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).
NITROGEN HETEROCYCLE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN HUMAN THERAPEUTICS
-
Paragraph 0229; 0230, (2013/03/26)
The present invention relates to compounds having general formula I characterised in that wherein in particular: R1 represents one or a plurality of groups such as: trifluoromethyl, halogen such as F, Cl, Br, methyl, nitro. R represents nitroge
