In 2016,Siebeneicher, Holger; Cleve, Arwed; Rehwinkel, Hartmut; Neuhaus, Roland; Heisler, Iring; Mueller, Thomas; Bauser, Marcus; Buchmann, Bernd published 《Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876》.ChemMedChem published the findings.Safety of Azetidin-3-ol hydrochloride The information in the text is summarized as follows:
Despite the long-known fact that the facilitative glucose transporter GLUT1 is one of the key players safeguarding the increase in glucose consumption of many tumor entities even under conditions of normal oxygen supply (known as the Warburg effect), only few endeavors have been undertaken to find a GLUT1-selective small-mol. inhibitor. Because other transporters of the GLUT1 family are involved in crucial processes, these transporters should not be addressed by such an inhibitor. A high-throughput screen against a library of ∼3 million compounds was performed to find a small mol. with this challenging potency and selectivity profile. The N-(1H-pyrazol-4-yl)quinoline-4-carboxamides were identified as an excellent starting point for further compound optimization. After extensive structure-activity relationship explorations, single-digit nanomolar inhibitors with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4 were obtained. The most promising compound, BAY-876 [N4-[1-(4-cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide], showed good metabolic stability in vitro and high oral bioavailability in vivo. In the experiment, the researchers used Azetidin-3-ol hydrochloride(cas: 18621-18-6Safety of Azetidin-3-ol hydrochloride)
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.Safety of Azetidin-3-ol hydrochloride Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts