Tripeptidyl-Peptidase II (TPP II) Inhibitory Activity of (S)-2,3-Dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a Systematic SAR Evaluation. Part 2

Autor:	Peter Walter Maria Roevens, Hans De Winter, Kavash Robert W, Michael Joseph Kukla, Maria V. F. Somers, Henry J. Breslin, Tamara A. Miskowski
Rok vydání:	2004
Předmět:	Serine protease biology Stereochemistry Chemistry biology.protein Tripeptidyl peptidase II General Medicine Pharmacophore Inhibitory postsynaptic potential IC50
Zdroj:	ChemInform. 35
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200412135
Popis:	We have systematically explored the structure–activity relationship (SAR) for a series of compounds 2 as inhibitors of tripeptidyl-peptidase II (TPP II), a serine protease responsible for the degradation of cholecystokinin-8 (CCK-8). This SAR evaluation of the core structure 2 suggest a fairly restrictive pharmacophore for such related structures, but has yielded a limited set of compounds (2b, 2c, 2d, 2s, and 2t) with potent TPP II inhibitory activity (IC50 4-11 nM).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::01d68875052e7e78e263510fd9ce94e6 https://doi.org/10.1002/chin.200412135 Zobrazit plný text záznamu Plný text