3-CHLORO-4-CARBOXAMIDO-6-ARYLPYRIDAZINES AS A NONPEPTIDE CLASS OF INTERLEUKIN-1-BETA CONVERTING-ENZYME-INHIBITOR

Authors
DOLLE RE HOYER D RINKER JM ROSS TM SCHMIDT SJ HELASZEK CT ATOR MA
Citation
Re. Dolle et al., 3-CHLORO-4-CARBOXAMIDO-6-ARYLPYRIDAZINES AS A NONPEPTIDE CLASS OF INTERLEUKIN-1-BETA CONVERTING-ENZYME-INHIBITOR, Bioorganic & medicinal chemistry letters, 7(8), 1997, pp. 1003-1006
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
8
Year of publication
1997
Pages
1003 - 1006
Database
ISI
SICI code
0960-894X(1997)7:8<1003:3AANCO>2.0.ZU;2-F
Abstract
The 3-chloro-4-carboxamido-6-arylpyridazines are a novel class of inte rleukin-1 beta converting enzyme (ICE) inhibitor. These agents are irr eversible inhibitors with pyridazine 23 possessing a k(obs)/[I] = 355 M-1 s(-1). A structure-activity relationship for this non-peptide clas s of compounds and the putative mechanism for irreversible inactivatio n are described. (C) 1997 Elsevier Science Ltd.