Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors

Autor:	Loran M. Killar, S. Skala, James M. Chen, X. Du, G. Jin, Roy A. Black, A. Zask, Michele A. Sharr, Gu Yansong, R. Cowling, C.J March, J.S. Skotnicki, J. D. Albright, Amy Sung, Dauphine Barone, John F. DiJoseph, C. E. Roth, Kendall M. Mohler, Jeremy I. Levin, M. Hogan
Rok vydání:	2003
Předmět:	Stereochemistry Clinical Biochemistry Pharmaceutical Science Biological Availability Matrix metalloproteinase ADAM17 Protein Matrix Metalloproteinase Inhibitors Hydroxamic Acids Biochemistry Chemical synthesis chemistry.chemical_compound Mice Structure-Activity Relationship In vivo Drug Discovery Pyrazolopyridine Animals Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Hydroxamic acid biology Bicyclic molecule Arthritis Organic Chemistry Metalloendopeptidases Bridged Bicyclo Compounds Heterocyclic Sulfonamide Rats ADAM Proteins Disease Models Animal Cartilage chemistry Enzyme inhibitor biology.protein Molecular Medicine Cattle
Zdroj:	Bioorganicmedicinal chemistry letters. 13(8)
ISSN:	0960-894X
Popis:	Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1' group. Select compounds were found to be effective in in vivo models of arthritis.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4826251a694d81522423585eb9f7e98 https://pubmed.ncbi.nlm.nih.gov/12668018 Zobrazit plný text záznamu Full Text from ScienceDirect