Referenced in: none

Automatically associated channels: Kir2.3

Title: The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.

Authors: Piyasena Hewawasam, Valentin K Gribkoff, Yadagiri Pendri, Steven I Dworetzky, Nicholas A Meanwell, Eduardo Martinez, Christopher G Boissard, Debra J Post-Munson, Joanne T Trojnacki, Krishnaswamy Yeleswaram, Lorraine M Pajor, Jay Knipe, Qi Gao, Robert Perrone, John E Starrett

Journal, date & volume: Bioorg. Med. Chem. Lett., 2002 Apr 8 , 12, 1023-6

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/11909708

Abstract
3-Aryl-3-fluorooxindoles can be efficiently synthesized in two steps by the addition of an aryl Grignard to an isatin, followed by treatment with DAST. Oxindole 1 (BMS-204352; MaxiPost) can be isolated using chiral HPLC or prepared by employing chiral resolution. Cloned maxi-K channels are opened by 1, which demonstrates a brain/plasma ratio >9 in rats.