Potent, orally bioavailable somatostatin agonists: Good absorption achieved by urea backbone cyclization

Article abstract of DOI:10.1016/S0960-894X(99)00016-5

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 acycyclic counterparts. SAP, studies subsequently led to highly potent analogs, selective for receptor subtype 2, and having good oral bioavailability.