Discovery of oxazole-based PDE4 inhibitors with picomolar potency

Autor:	Pauline C. Ting, Motasim Billah, Ji Zhang, Peng Wang, Daniel Prelusky, David J. Blythin, John H. Schwerdt, John J. Piwinski, Ling Lin, Li Xiao, Xiao Chen, Xiang Zhang, Ho-Jane Shue, Neng-Yang Shih, Jianhua Cao, Ping Wu, Chander S. Celly, Rongze Kuang, Robert G. Aslanian, Danlin Gu
Rok vydání:	2011
Předmět:	Models Molecular Stereochemistry Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science Biochemistry Cyclic N-Oxides chemistry.chemical_compound Structure-Activity Relationship Phosphodiesterase-4 In vivo Drug Discovery Potency Animals Humans PDE4 Inhibitors Molecular Biology Oxazoles Oxazole Tumor Necrosis Factor-alpha Organic Chemistry Biological activity Cyclic Nucleotide Phosphodiesterases Type 4 Rats chemistry Quinolines Molecular Medicine Phosphodiesterase 4 Inhibitors Selectivity
Zdroj:	Bioorganicmedicinal chemistry letters. 22(7)
ISSN:	1464-3405
Popis:	Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-α-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity profiles and in vivo biological activity are also reported.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76ef660ee57e97c99ba25220cea0146f https://pubmed.ncbi.nlm.nih.gov/22401864 Zobrazit plný text záznamu Full Text from ScienceDirect