Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

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

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

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Article Details

VOLUME: 1
ISSUE: 1
Year: 2004
Page: [84 - 87]
Pages: 4
DOI: 10.2174/1570180043485761