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7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.

Abstract：

:High-throughput file screening against inhibition of human lung PDE4 led to the discovery of 3-ethyl-1-(4-fluorophenyl)-6-phenyl-7-oxo-4, 5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine (11) as a novel PDE4 inhibitor. Subsequent SAR development, using an eosinophil PDE assay, led to analogues up to 50-fold more potent than 11 with IC50 values of 0.03-1.6 microM. One such compound, CP-220,629 (22) (IC50 = 0.44 microM), was efficacious in the guinea pig aerosolized antigen induced airway obstruction assay (ED50 2.0 mg/kg, po) and demonstrated a significant reduction in eosinophil (55%), neutrophil (65%), and IL-1beta (82%) responses to antigen challenge in atopic monkeys (10 mg/kg, po).

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Duplantier AJ,Andresen CJ,Cheng JB,Cohan VL,Decker C,DiCapua FM,Kraus KG,Johnson KL,Turner CR,UmLand JP,Watson JW,Wester RT,Williams AS,Williams JA

doi

10.1021/jm9800090

subject

Has Abstract

pub_date

1998-06-18 00:00:00

pages

2268-77

issue

13

eissn

0022-2623

issn

1520-4804

pii

jm9800090

journal_volume

41

pub_type

杂志文章

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