Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors

Autor:	Lee Tai Liu, Shyh-Fong Chen, Chou Shan-Yen, Ying-Ta Wu, Tom S. Chen, Li-Rung Chen, Yi Wen Lin, Chih-Jung Kuo, Shin-Hun Juang, Yu-Chin Wang
Rok vydání:	2005
Předmět:	Isatin SARS CoV protease inhibitor medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science medicine.disease_cause Biochemistry Substrate Specificity chemistry.chemical_compound Papain Drug Discovery Fluorescence Resonance Energy Transfer Chymotrypsin Trypsin skin and connective tissue diseases Coronavirus 3C Proteases Coronavirus Molecular Structure biology Cysteine Endopeptidases Severe acute respiratory syndrome-related coronavirus Molecular Medicine psychological phenomena and processes medicine.drug Proteases Stereochemistry education Article Structure-Activity Relationship Viral Proteins Endopeptidases medicine Humans Computer Simulation Protease Inhibitors Protease inhibitor (pharmacology) Molecular Biology Binding Sites Protease fungi Organic Chemistry body regions Enzyme Activation chemistry biology.protein
Zdroj:	Bioorganic & Medicinal Chemistry Letters
ISSN:	0960-894X
Popis:	Graphical abstract N-Substituted isatin derivatives have been prepared and their inhibition activities against SARS viral protease were evaluated. N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::205cb7fb3a4251b5c88984d5232bbb40 https://doi.org/10.1016/j.bmcl.2005.04.027 Zobrazit plný text záznamu Full Text from ScienceDirect