Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
Basic Information
ID: ALA1136389
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
Authors: Turner SC, Carroll WA, White TK, Brune ME, Buckner SA, Gopalakrishnan M, Fabiyi A, Coghlan MJ, Scott VE, Castle NA, Daza AV, Milicic I, Sullivan JP.
Abstract: We have discovered a novel series of N-[2-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-naphthalen-1-yl] amides that are potent openers of K(ATP) channels and investigated structure-activity relationships (SAR) around the 1,2-disubstituted naphthyl core. A-151892, a prototype compound of this series, was found to be a potent and efficacious potassium channel opener in vitro in transfected Kir6.2/SUR2B cells and pig bladder strips. Additionally, A-151892 was found to selectively inhibit unstable bladder contractions in vivo in an obstructed rat model of myogenic bladder function
CiteXplore: 12729655
DOI: 10.1016/s0960-894x(03)00205-1
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