Synthesis and characterization of novel pyridine associated 1,2,4-triazolo-1,3,4-thiadiazines
A series of novel 3-(1-methyl-1H-pyrazol-4-yl)-6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadaizine and its derivatives (8a-f) were synthesized by using 1-methyl-1H-pyrazole-4-carboxylic acid (3) as starting material and by involving 1-methyl-1H-pyrazole-
HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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Paragraph 0668; 0674
(2018/06/12)
Narrow SAR in odorant sensing Orco receptor agonists
The systematic exploration of a series of triazole-based agonists of the cation channel insect odorant receptor is reported. The structure-activity relationships of independent sections of the molecules are examined. Very small changes to the compound structure were found to exert a large impact on compound activity. Optimal substitutions were combined using a 'mix-and-match' strategy to produce best-in-class compounds that are capable of potently agonizing odorant receptor activity and may form the basis for the identification of a new mode of insect behavior modification.
Romaine, Ian M.,Taylor, Robert W.,Saidu, Samsudeen P.,Kim, Kwangho,Sulikowski, Gary A.,Zwiebel, Laurence J.,Waterson, Alex G.
p. 2613 - 2616
(2014/06/09)
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