Synthesis and evaluation of CE-0266: A new human neutrophil elastase inhibitor

Autor:	Qi-Long Ying, Suzanne E. Mangold, Sherman E. Ross, Lyle W. Spruce, Sanford R. Simon, Raymond T. Cunningham, John C. Cheronis, Gary P. Kirschenheuter, Maciej Wieczorek
Rok vydání:	1992
Předmět:	biology Stereochemistry Organic Chemistry Elastase Butyrate Granulocyte Biochemistry Chemical synthesis Sulfone chemistry.chemical_compound Elastase inhibitor medicine.anatomical_structure chemistry In vivo Enzyme inhibitor Drug Discovery medicine biology.protein Molecular Biology
Zdroj:	Bioorganic Chemistry. 20:345-355
ISSN:	0045-2068
DOI:	10.1016/0045-2068(92)90044-4
Popis:	The synthesis and evaluation of 4-(methylsulfinyl)phenyl 2-(1-methyl-2-pyrrolyl)butyrate (CE-0266) and the related sulfide and sulfone derivatives, CE-0265 and CE-0267, respectively, are described. The potency of the inhibitors toward human neutrophil elastase increases across the series CE-0265, CE-0266, CE-0267. CE-0266, with a k3Ki∗k2 value of 36 nm, exhibited high selectivity for elastase and was chosen for additional in vivo studies.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::9f521790e5911eab642fbae00198ea40 https://doi.org/10.1016/0045-2068(92)90044-4 Zobrazit plný text záznamu