Elsevier, Bioorganic and Medicinal Chemistry Letters, 2(12), p. 109-112
DOI: 10.1016/s0960-894x(01)00630-8
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Replacement of the 2-Adoc-D-alphaMeTrp residue in the non-selective CCK(1) receptor agonist PD 170292 by the Z-(2R,5R,11bS)-IBTM skeleton, able to fix a type II beta-turn-like conformation, led to a conformationally restricted dipeptoid analogue, namely 3a, which exhibited a notable increase in the CCK(1) selectivity and antagonist properties.