REDUCED AMIDE BOND NEUROTENSIN-8-13 MIMETICS WITH POTENT IN-VIVO ACTIVITY

Authors
WUSTROW DJ DAVIS MD AKUNNE HC CORBIN AE WILEY JN WISE LD HEFFNER TG
Citation
Dj. Wustrow et al., REDUCED AMIDE BOND NEUROTENSIN-8-13 MIMETICS WITH POTENT IN-VIVO ACTIVITY, Bioorganic & medicinal chemistry letters, 5(9), 1995, pp. 997-1002
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
9
Year of publication
1995
Pages
997 - 1002
Database
ISI
SICI code
0960-894X(1995)5:9<997:RABNMW>2.0.ZU;2-R
Abstract
Appropriately substituted 8-9 (Psi CH2NH) isosteres of neurotensin (NT ) 8-13 have been found which are active as NT agonists in vitro and in vivo. SAR studies suggest that preventing amide bond hydrolysis at th e 8-9 and 11-12 positions of NT(8-13) mimetics is important for produc ing compounds with potent activity in vivo. Other simplified replaceme nts for the Arg-Arg portion of NT(8-13) are reported.