1, 4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma
SB Christensen, A Guider, CJ Forster…
Index: Christensen, Siegfried B.; Guider, Aimee; Forster, Cornelia J.; Gleason, John G.; Bender, Paul E.; Karpinski, Joseph M.; Dewolf Jr., Walter E.; Barnette, Mary S.; Underwood, David C.; Griswold, Don E.; Cieslinski, Lenora B.; Burman, Miriam; Bochnowicz, Steven; Osborn, Ruth R.; Manning, Carol D.; Grous, Marilyn; Hillegas, Leonard M.; Bartus, Joan O'Leary; Dominic Ryan; Eggleston, Drake S.; Curtis Haltiwanger; Torphy, Theodore J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 6 p. 821 - 835
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Citation Number: 147
Abstract
Evaluation of a variety of PDE4 inhibitors in a series of cellular and in vivo assays suggested a strategy to improve the therapeutic index of PDE4 inhibitors by increasing their selectivity for the ability to inhibit PDE4 catalytic activity versus the ability to compete for high affinity [3H] rolipram-binding sites in the central nervous system. Use of this strategy led ultimately to the identification of cis-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl] cyclohexane-1- ...
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