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

A. M. Crider; S. Liu; T. Li; S. Mahajan; M. Ankersen; C. E. Stidsen

doi:10.2174/1570180043485761

ISSN: 1570-1808
E-ISSN: 1875-628X

Somatostatin Receptor Subtype 4 (sst4) Ligands: Synthesis and Evaluation of Indol-3-yl- and 2-Pyridyl-Thioureas
Authors: A. M. Crider¹, S. Liu², T. Li³, S. Mahajan⁴, M. Ankersen⁵ and C. E. Stidsen⁶
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¹ Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209, USA. ² Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209, USA. ³ Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209, USA. ⁴ Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209, USA. ⁵ Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209, USA. ⁶ Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209, USA.
Source: Letters in Drug Design & Discovery, Volume 1, Issue 1, Jan 2004, p. 84 - 87
DOI: https://doi.org/10.2174/1570180043485761
- Available online: 01 Jan 2004

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.

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2004-01-01

2025-09-30

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Article Type: Review Article

Keyword(s): binding affinity; imidazol-4-yl; propyl group; somatostatin; somatostatin receptors; thioureas

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

Abstract

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