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. 2003 May 19;13(10):1741-4.
doi: 10.1016/s0960-894x(03)00205-1.

Structure-activity relationship of a novel class of naphthyl amide KATP channel openers

Sean C Turner  1 , William A Carroll, Tammie K White, Michael E Brune, Steven A Buckner, Murali Gopalakrishnan, Adebola Fabiyi, Michael J Coghlan, Victoria E Scott, Neil A Castle, Anthony V Daza, Ivan Milicic, James P Sullivan
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Structure-activity relationship of a novel class of naphthyl amide KATP channel openers

Sean C Turner et al. Bioorg Med Chem Lett. .

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

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