TY - JOUR
T1 - New orally active PDE4 inhibitors with therapeutic potential
AU - Ochiai, Hiroshi
AU - Ishida, Akiharu
AU - Ohtani, Tazumi
AU - Kusumi, Kensuke
AU - Kishikawa, Katuya
AU - Yamamoto, Susumu
AU - Takeda, Hiroshi
AU - Obata, Takaaki
AU - Nakai, Hisao
AU - Toda, Masaaki
PY - 2004/8/1
Y1 - 2004/8/1
N2 - The design, synthesis, and biological evaluation of a series of pyrazolopyridines was carried out. Structural optimization of the aniline moiety of 4-anilinopyrazolopyridine derivative 3a, which is one of the newly discovered chemical leads for PDE4 inhibitors from our in-house library, was performed successfully. The details of the discovery of new orally active PDE4 inhibitors, which are expected to show therapeutic potential, are presented and their structure-activity relationships are discussed. Pharmacological evaluation and pharmacokinetic data for representative compounds are also presented.
AB - The design, synthesis, and biological evaluation of a series of pyrazolopyridines was carried out. Structural optimization of the aniline moiety of 4-anilinopyrazolopyridine derivative 3a, which is one of the newly discovered chemical leads for PDE4 inhibitors from our in-house library, was performed successfully. The details of the discovery of new orally active PDE4 inhibitors, which are expected to show therapeutic potential, are presented and their structure-activity relationships are discussed. Pharmacological evaluation and pharmacokinetic data for representative compounds are also presented.
KW - 4-Anilinopyrazolopyridine
KW - Orally active
KW - PDE4 inhibitor
UR - http://www.scopus.com/inward/record.url?scp=3042793387&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=3042793387&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2004.05.032
DO - 10.1016/j.bmc.2004.05.032
M3 - Article
C2 - 15246087
AN - SCOPUS:3042793387
VL - 12
SP - 4089
EP - 4100
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 15
ER -