Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

Autor:	Teresa Brooks, Richard Faint, Sukhjit Sohal, Adrian Folkes, Golec Julian M C, Peter Charlton, Michael Bryan Roe
Rok vydání:	2001
Předmět:	chemistry.chemical_classification medicine.drug_class Stereochemistry Carboxylic acid Organic Chemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Diketopiperazines Biochemistry Chemical synthesis Thiophene derivatives Piperazines In vitro Structure-Activity Relationship chemistry.chemical_compound chemistry Plasminogen activator inhibitor-1 Plasminogen Activator Inhibitor 1 Drug Discovery medicine Lactam Molecular Medicine Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 11:2589-2592
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(01)00508-x
Popis:	We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC 50 =0.2 μM. The synthesis and SAR of these compounds are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::766e7b20a095c6f68d57e64459468757 https://doi.org/10.1016/s0960-894x(01)00508-x Zobrazit plný text záznamu Full Text from ScienceDirect