Discovery of new orally active phosphodiesterase (PDE4) inhibitors

…, A Ishida, T Ohtani, K Kusumi, K Kishikawa…

Index: Ochiai, Hiroshi; Ishida, Akiharu; Ohtani, Tazumi; Kusumi, Kensuke; Kishikawa, Katuya; Yamamoto, Susumu; Takeda, Hiroshi; Obata, Takaaki; Nakai, Hisao; Toda, Masaaki Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 9 p. 1098 - 1104

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Citation Number: 15

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 ...

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