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

Autor: Crider, A. M., Liu, S., Li, T., Mahajan, S., Ankersen, M., Stidsen, C. E.
Zdroj: Letters in Drug Design & Discovery; January 01, 2004, Vol. 1 Issue: 1 p84-87, 4p
Abstrakt: 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.
Databáze: Supplemental Index