Title
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
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Oxford ,
Subject
Chemistry
Pharmacology. Therapy
Source (journal)
Bioorganic and medicinal chemistry letters. - Oxford
Volume/pages
13(2003) :24 , p. 4467-4471
ISSN
0960-894X
0960-894X
ISI
000187010700043
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Abstract
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). (C) 2003 Elsevier Ltd. All rights reserved.
E-info
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