MilliporeSigma

Discovery of new orally active phosphodiesterase (PDE4) inhibitors.

Chemical & pharmaceutical bulletin (2004-09-02)
Hiroshi Ochiai, Akiharu Ishida, Tazumi Ohtani, Kensuke Kusumi, Katuya Kishikawa, Susumu Yamamoto, Hiroshi Takeda, Takaaki Obata, Hisao Nakai, Masaaki Toda
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
5-Amino-1,3-dimethylpyrazole, 97%