Thiourea analogues of NNC 26-9100 (2) were prepared as somatostatin receptor subtype 4 (sst4) ligands. The indole 9 exhibited high affinity (Ki = 23 nM) and about a 100-fold selectivity at sst4 compared to sst2 receptors. The (imidazol-4-yl) propyl group appears to play a major role in the affinity and selectivity of these thioureas at sst4.
Keywords: thioureas, somatostatin, somatostatin receptors, imidazol-4-yl, propyl group, binding affinity
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