Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 20, Pages 6133-6137Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm051222g
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A benzodiazepine-based beta-turn mimetic has been designed, synthesized, and incorporated into angiotensin II. Comparison of the mimetic with beta-turns in crystallized proteins showed that it most closely resembles a type II beta-turn. The compounds exhibited high to moderate binding affinity for the AT(2) receptor, and one also displayed high affinity for the AT(1) receptor. Molecular modeling showed that the high-affinity compounds could be incorporated into a previously derived model of AT(2) receptor ligands.
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