Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis

Autor:	Dirk Heimbach, Stefan Weigand, Johannes-Peter Stasch, Michael Brands, Jens-Kerim Ergueden, Kentaro Hashimoto, Stephan Siegel, Christian Schroeder
Rok vydání:	2005
Předmět:	Indoles Stereochemistry Endothelin converting enzyme 1 High-throughput screening Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Endothelin-Converting Enzymes Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship Lead (geology) Phase (matter) Drug Discovery Side chain Aspartic Acid Endopeptidases Combinatorial Chemistry Techniques Humans Enzyme Inhibitors education Molecular Biology chemistry.chemical_classification Indole test education.field_of_study biology Organic Chemistry Metalloendopeptidases General Medicine Combinatorial chemistry Sulfonamide chemistry Enzyme inhibitor biology.protein Molecular Medicine Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:4201-4205
ISSN:	0960-894X
Popis:	A novel class of indole-based endothelin-converting enzyme (ECE) inhibitors was identified by high throughput screening. We report systematic optimization of this compound class by means of classical and solid-phase chemistry. Optimized compounds with a bisarylamide side chain at the 2-position of the indole skeleton exhibit low-nanomolar activity on ECE.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8f2bb8b4784403505390202d28b1ecb https://doi.org/10.1016/j.bmcl.2005.06.085 Zobrazit plný text záznamu Full Text from ScienceDirect