The search for novel nonpeptide somatostatin (SST) agonists has been the focus of our laboratory for over 15 years.. SST levels are known to be depressed in the brain cortex and hippocampus of Alzheimer's disease patients. These brain areas contain a high level of expression of sst4 receptors. Although NNC 26-9100, the first nonpeptide reported, has been shown to increase memory and learning in mice, we have a continued interest in developing new scaffolds with potential therapeutic use in AD. 1,2,4-Triazoles are readily synthesized by a reported method in which thioamides are condensed with hydrazides in the presence of silver benzoate to facilitate ring closure. The resulting derivatives are metabolic stable and diversified at three positions. Although most of the 1,2,4-triazoles showed only weak binding affinity at sst4,  a triazole bearing an (imidazol-4-yl)propyl group at the 1-position of the nucleus demonstrated several fold higher affinity at sst4 than NNC 26-9100

Synthesis of trisubstituted-1,2,4-triazoles as somatostatin subtype-4 receptor (sst<sub>4</sub>) ligands

243rd National Meeting (2012)

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Synthesis of trisubstituted-1,2,4-triazoles as somatostatin subtype-4 receptor (sst4) ligands

Synthesis of trisubstituted-1,2,4-triazoles as somatostatin subtype-4 receptor (sst₄) ligands