Yang, Wu published the artcileDiscovery of 4-Aryl-7-Hydroxyindoline-Based P2Y1 Antagonists as Novel Antiplatelet Agents, Recommanded Product: 5-Chlorothiazolo[5,4-b]pyridin-2-amine, the publication is Journal of Medicinal Chemistry (2014), 57(14), 6150-6164, database is CAplus and MEDLINE.
ADP (ADP)-mediated platelet aggregation is signaled through two distinct G protein-coupled receptors (GPCR) on the platelet surface: P2Y12 and P2Y1. Blocking P2Y12 receptor is a clin. well-validated strategy for antithrombotic therapy. P2Y1 antagonists have been shown to have the potential to provide equivalent antithrombotic efficacy as P2Y12 inhibitors with reduced bleeding in preclin. animal models. Th have previously reported the discovery of a potent and orally bioavailable P2Y1 antagonist, I. This paper describes further optimization of I by introducing 4-aryl groups at the hydroxylindoline in two series. In the neutral series, II was identified with excellent potency and desirable pharmacokinetic (PK) profile. It also demonstrated similar antithrombotic efficacy with less bleeding compared with the known P2Y12 antagonist prasugrel in rabbit efficacy/bleeding models. In the basic series, III (BMS-884775) was discovered with an improved PK and liability profile over I. These results support P2Y1 antagonism as a promising new antiplatelet target.
Journal of Medicinal Chemistry published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C9H10O4, Recommanded Product: 5-Chlorothiazolo[5,4-b]pyridin-2-amine.
Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica