In 2010,Palmer, Andreas M.; Chiesa, Vittoria; Schmid, Anja; Muench, Gabriela; Grobbel, Burkhard; Zimmermann, Peter J.; Brehm, Christof; Buhr, Wilm; Simon, Wolfgang-Alexander; Kromer, Wolfgang; Postius, Stefan; Volz, Jurgen; Hess, Dietmar published 《Tetrahydrochromenoimidazoles as Potassium-Competitive Acid Blockers (P-CABs): Structure – Activity Relationship of Their Antisecretory Properties and Their Affinity toward the hERG Channel》.Journal of Medicinal Chemistry published the findings.Electric Literature of C3H8ClNO The information in the text is summarized as follows:
Potassium-competitive acid blockers constitute a new therapeutic option for the treatment of acid-related diseases that are widespread and constitute a significant economical burden. Enantiomerically pure (tetrahydro)chromenoimidazoles I [R1 = 2-MeC6H4, R2 = Et, R3 = H; R1 = 2-(c-C3H5)C6H4, R2 = R3 = Me, etc.] were prepared using either the readily available candidate I (R1 = 2-MeC6H4, R2 = R3 = Me) as starting material or where the Noyori asym. reduction of ketones, e.g., II, was the key reaction. A comprehensive SAR regarding the influence of the 5-carboxamide and the 8-aryl residue on in vitro activity, acid-suppression in the Ghosh Schild rat, and affinity toward the hERG channel was established. In addition, efficacy and duration of the antisecretory action was examined for the most promising target compounds by 24 h pH-metry in the fistula dog and a significantly different SAR was observed as compared to the Ghosh Schild rat. Several (tetrahydro)chromenoimidazoles were identified that possessed a comparable profile as the candidate I (R1 = 2-MeC6H4, R2 = R3 = Me). In the part of experimental materials, we found many familiar compounds, such as Azetidin-3-ol hydrochloride(cas: 18621-18-6Electric Literature of C3H8ClNO)
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.Electric Literature of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
Referemce:
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