Thiazole-diamides as potent gamma-secretase inhibitors

Autor:	Christine E. Oborski, Kevin Cherry, Barbara-Anne Martin, Barbara G. Sahagan, Yuhpyng L. Chen, Michael L. Corman, Chandra B. Gamlath, Dane R. Liston, Charles F. Ebbinghaus
Rok vydání:	2007
Předmět:	Magnetic Resonance Spectroscopy Alkylation Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide macromolecular substances Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Amyloid precursor protein Thiazole Molecular Biology Amination chemistry.chemical_classification Diamide biology Cell-Free System Molecular Structure Organic Chemistry In vitro Thiazoles Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine Amyloid Precursor Protein Secretases Amyloid precursor protein secretase
Zdroj:	Bioorganicmedicinal chemistry letters. 17(20)
ISSN:	0960-894X
Popis:	The thiazole-diamide series (1) has been identified as highly potent gamma-secretase inhibitors. Several representative compounds showed IC(50) values of0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [(3)H]-2a, are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34abb697dd90d55365032c52c3f06648 https://pubmed.ncbi.nlm.nih.gov/17764937 Zobrazit plný text záznamu Full Text from ScienceDirect