Tetrahydrochromenoimidazoles as Potassium-Competitive Acid Blockers (P-CABs): Structure – Activity Relationship of Their Antisecretory Properties and Their Affinity toward the hERG Channel was written by 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. And the article was included in Journal of Medicinal Chemistry in 2010.Category: alcohols-buliding-blocks This article mentions the following:
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 experiment, the researchers used many compounds, for example, 1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3Category: alcohols-buliding-blocks).
1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3) belongs to alcohols. Because alcohols are easily synthesized and easily transformed into other compounds, they serve as important intermediates in organic synthesis. Alcohols may be oxidized to give ketones, aldehydes, and carboxylic acids. These functional groups are useful for further reactions. Oxidation of organic compounds generally increases the number of bonds from carbon to oxygen (or another electronegative element, such as a halogen), and it may decrease the number of bonds to hydrogen.Category: alcohols-buliding-blocks
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts