title: Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.
abstract: Backbone cyclization of urea-based somatostatin agonists resulted in novel, orally bioavailable agonists. Binding assays confirmed that the resulting conformationally constrained cyclic ureas retained the potency of their acyclic counterparts. SAR studies subsequently led to highly potent analogs, selective for receptor subtype 2, and having good oral bioavailability.
authors: Department of Medicinal Chemistry, and Biochemistry & Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors: A
authors: A
authors: Pasternak
authors: Y
authors: Y
authors: Pan
authors: D
authors: D
authors: Marino
authors: P E
authors: PE
authors: Sanderson
authors: R
authors: R
authors: Mosley
authors: S P
authors: SP
authors: Rohrer
authors: E T
authors: ET
authors: Birzin
authors: S E
authors: SE
authors: Huskey
authors: T
authors: T
authors: Jacks
authors: K D
authors: KD
authors: Schleim
authors: K
authors: K
authors: Cheng
authors: J M
authors: JM
authors: Schaeffer
authors: A A
authors: AA
authors: Patchett
authors: L
authors: L
authors: Yang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001562:Benzimidazoles; D001682:Biological Availability; D004285:Dogs; D007211:Indoles; D013004:Somatostatin / Q000819:agonists* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry*
chemical_list: D001562:Benzimidazoles; D007211:Indoles; C114420:L 054522; D013004:Somatostatin; D014508:Urea