Nonpeptide somatostatin agonists with sst4 selectivity: Synthesis and structure-activity relationships of thioureas

…, C Tang, B Ho, M Ankersen, CE Stidsen…

Index: Liu, Shenquan; Tang, Cheng; Ho, Bin; Ankersen, Michael; Stidsen, Carsten E.; Crider, A. Michael Journal of Medicinal Chemistry, 1998 , vol. 41, # 24 p. 4693 - 4705

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Citation Number: 61

Abstract

Utilizing NNC 26-9100 (11) as a structural lead, a variety of nonpeptide derivatives of somatostatin were synthesized and evaluated for sst2 and sst4 receptor binding affinity. A novel thiourea scaffold was utilized to attach (1) a heteroaromatic nucleus to mimic the Trp8 residue,(2) a nonheteroaromatic nucleus to mimic Phe7, and (3) a primary amine or other basic group to mimic the Lys9 residue of somatostatin. Displacement studies were carried ...