Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation

Authors
Souers, AJ Rosenquist, A Jarvie, EM Ladlow, M Feniuk, W Ellman, JA
Citation
Aj. Souers et al., Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation, BIOORG MED, 10(24), 2000, pp. 2731-2733
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
24
Year of publication
2000
Pages
2731 - 2733
Database
ISI
SICI code
0960-894X(200012)10:24<2731:OOASMV>2.0.ZU;2-5
Abstract
Constrained analogues 5-7 of the potent and subtype selective somatostatin mimetic 1 were prepared by incorporating conformational constraints into th e nine-membered heterocyclic scaffold. Each constrained peptidomimetic show ed an altered activity profile relative to lead compound 1, with compound 7 exhibiting a 25-fold and 2-fold binding enhancement against somatostatin r eceptor subtypes sst4 and sst5, respectively. (C) 2000 Elsevier Science Ltd . All rights reserved.