Young, Summer E. published the artcileSynthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets, SDS of cas: 321438-86-2, the main research area is proteinase activated receptor PAR4.
Protease activated receptor-4 [PAR4, proteinase-activated receptor PAR-4] is one of thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. The authors sought to develop potent, selective and novel PAR4 antagonists to test the role of PAR4 in thrombosis and hemostasis. The development of an expedient three-step synthetic route to access a novel series of indole-based PAR4 antagonists also necessitated the development of a platelet based high-throughput screening assay. Screening and subsequent structure activity relationship anal. yielded several selective PAR4 antagonists as well as possible new scaffolds for future antagonist development. The title compounds thus formed included an indole benzoic acid ester (I) and related substances. I was evaluated against an indazole benzoic acid ester analog (II) [i.e., 4-[1-(phenylmethyl)-1H-indazol-3-yl]benzoic acid Et ester]. The synthesis of the target compounds was achieved using 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole as starting materials. The synthetic sequence involved an alkylation of 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole, formation of bromide derivatives and a subsequent coupling reaction with boronic acids.
PLoS One published new progress about Allosterism. 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, SDS of cas: 321438-86-2.