2003 Medicinal chemistry

Medicinal chemistryV 1100 Novel Openers of Ca2+-Dependent Large-Conductance Potassium Channels:

Symmetrical Pharmacophore and Electrophysiological Evaluation of Bisphenols. — A bioisosteric approach by replacing the amide moiety of the maxi-K opener NS-004 by a phenolic OH as well as exploring the pseudo-symmetrical elements of NS-004 lead to the discovery of bisphenols (I)—(III) as openers of cloned maxi-K channels expressed in oocytes. — (LI*, Y.; JOHNSON, G.; ROMINE, J. L.; MEANWELL, N. A.; MARTIN, S. W.; DWORETZKY, S. I.; BOISSARD, C. G.; GRIBKOFF, V. K.; STARRETT, J. E. J.; Bioorg. Med. Chem. Lett. 13 (2003) 8, 1437-1439; Bristol-Myers Squibb Pharm. Res. Inst., Wallingford, CT 06492, USA; Eng.) — H. Hoennerscheid

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