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Letters in Drug Design & Discovery

Author(s): A. M. Crider, S. Liu, T. Li, S. Mahajan, M. Ankersen and C. E. Stidsen

DOI: 10.2174/1570180043485761

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Somatostatin Receptor Subtype 4 (sst4) Ligands: Synthesis and Evaluation of Indol-3-yl- and 2-Pyridyl-Thioureas

Page: [84 - 87] Pages: 4

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Abstract

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