Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives

Autor:	Pierre Danhaive, Laurent Provins, Jacques Dulieu, Karin J. Stebbins, Luc Quere, Michel Gillard, Bernard Christophe
Rok vydání:	2007
Předmět:	Pyrimidine Stereochemistry Guinea Pigs Clinical Biochemistry Azetidine Pharmaceutical Science Biochemistry Chemical synthesis Mice Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Animals Humans PDE4 Inhibitors Molecular Biology Receptor Muscarinic M3 Mice Inbred BALB C biology Chemistry Pulmonary inflammation Organic Chemistry Cyclic Nucleotide Phosphodiesterases Type 4 Pyrimidines 3' 5'-Cyclic-AMP Phosphodiesterases Enzyme inhibitor Lung disease biology.protein Azetidines Molecular Medicine Female
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:3077-3080
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2007.03.047
Popis:	Introduction of 3-substituted azetidinyl substituents onto the 4,6-diaminopyrimidine scaffold allowed the improvement of PDE4 inhibiting activities. Preliminary in vivo activity in pulmonary inflammation models is reported.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c797927517c7c8fc2ec2198e1dc15c0c https://doi.org/10.1016/j.bmcl.2007.03.047 Zobrazit plný text záznamu Full Text from ScienceDirect