In 2016,Johansson, Anders; Loefberg, Christian; Antonsson, Madeleine; von Unge, Sverker; Hayes, Martin A.; Judkins, Robert; Ploj, Karolina; Benthem, Lambertus; Linden, Daniel; Brodin, Peter; Wennerberg, Marie; Fredenwall, Marlene; Li, Lanna; Persson, Joachim; Bergman, Rolf; Pettersen, Anna; Gennemark, Peter; Hogner, Anders published 《Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties》.Journal of Medicinal Chemistry published the findings.Related Products of 18621-18-6 The information in the text is summarized as follows:
A novel series of melanin concentrating hormone receptor 1 (MCHr1) antagonists were the starting point for a drug discovery program that culminated in the discovery of 103 (AZD1979). The lead optimization program was conducted with a focus on reducing lipophilicity and understanding the physicochem. properties governing CNS exposure and undesired off-target pharmacol. such as hERG interactions. An integrated approach was taken where the key assay was ex vivo receptor occupancy in mice. The candidate compound 103 displayed appropriate lipophilicity for a CNS indication and showed excellent permeability with no efflux. Preclin. GLP toxicol. and safety pharmacol. studies were without major findings and 103 was taken into clin. trials. In the experiment, the researchers used Azetidin-3-ol hydrochloride(cas: 18621-18-6Related Products of 18621-18-6)
Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Related Products of 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
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