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Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs.

1997; Elsevier BV; Volume: 7; Issue: 3 Linguagem: Inglês

10.1016/s0960-894x(96)00623-3

1464-3405

Siem J. Veenstra, Kathleen Hauser, Claudia Betschart,

Pharmacological Receptor Mechanisms and Effects

Five conformationally restricted analogs of CGP 49823 have been synthesized. Comparison of their in vitro activities indicates an active conformation of CGP 49823 in which the two aromatic rings of the benzyl and the benzoyl groups are in proximity of each other.