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Chemical & pharmaceutical bulletin

Discovery of new orally active phosphodiesterase (PDE4) inhibitors.


PMID 15340197

Abstract

A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.

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532223
5-Amino-1,3-dimethylpyrazole, 97%
C5H9N3