Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Discovery of New Orally Active Phosphodiesterase (PDE4) Inhibitors
Hiroshi OchiaiAkiharu IshidaTazumi OhtaniKensuke KusumiKatuya KishikawaSusumu YamamotoHiroshi TakedaTakaaki ObataHisao NakaiMasaaki Toda
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2004 Volume 52 Issue 9 Pages 1098-1104

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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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© 2004 The Pharmaceutical Society of Japan
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