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ID: ALA1132396
Journal: Bioorg Med Chem Lett
Title: Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.
Authors: Pasternak A, Pan Y, Marino D, Sanderson PE, Mosley R, Rohrer SP, Birzin ET, Huskey SE, Jacks T, Schleim KD, Cheng K, Schaeffer JM, Patchett AA, Yang L.
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.
CiteXplore: 10091708