Phenyl piperidine-based orally active peptidomimetic agonists for somatostatin receptor subtype-2

Selective human somatostatin subtype-2 (hsst2) receptor agonists have received considerable attention recently since they may offer benefit in treating diabetes [1]. Specifically, sst2 activation inhibits growth hormone (GH) and glucagon release without much effect on the release of insulin. Cyclic peptide 1 and small molecule 2 [1] represent selective ligands for hsst2. In this paper we disclose orally active phenyl piperidine-based small molecule agonists which possess high selectivity towards hsst2.