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Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.

作者信息

Hulme C, Poli G B, Huang F C, Souness J E, Djuric S W

机构信息

Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.

出版信息

Bioorg Med Chem Lett. 1998 Jan 20;8(2):175-8. doi: 10.1016/s0960-894x(97)10206-2.

Abstract

The following letter presents the synthesis and in vitro evaluation of a novel quaternary substituted series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds represent conformationally constrained analogues of the Celltech PDE IV inhibitor, CDP 840. Examples with sub-micromolar IC50's for PDE4 inhibition are reported.

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