|
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
|
|
|
|
|
|
|
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. |
|
|
|
Language
|
|
|
|
English
|
|
|
Source (journal)
|
|
|
|
Bioorganic and medicinal chemistry letters. - Oxford
|
|
|
Publication
|
|
|
|
Oxford
:
2003
|
|
|
ISSN
|
|
|
|
0960-894X
|
|
|
DOI
|
|
|
|
10.1016/J.BMCL.2003.09.014
|
|
|
Volume/pages
|
|
|
|
13
:24
(2003)
, p. 4467-4471
|
|
|
ISI
|
|
|
|
000187010700043
|
|
|
Full text (Publisher's DOI)
|
|
|
|
|
|
|
Full text (publisher's version - intranet only)
|
|
|
|
|
|