Journal of Medicinal Chemistry p. 821 - 835 (1998)
Update date:2022-08-05
Topics:
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.
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-carboxylic acid (1, SB 207499, Ariflo(TM)), a potent second-generation inhibitor of PDE4 with a decreased potential for side effects versus the archetypic first generation inhibitor, (R)-rolipram.
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Doi:10.1016/S0040-4039(01)01439-3
(2001)Doi:10.1039/jr9520003281
(1952)Doi:10.1246/bcsj.71.459
(1998)Doi:10.1039/a704248e
(1998)Doi:10.1039/j39680002221
(1968)Doi:10.1016/S0040-4039(03)00471-4
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