Chemical and Pharmaceutical Bulletin p. 1631 - 1641 (1997)
Update date:2022-08-05
Topics:
Yamada, Yasuki
Ando, Koji
Ikemoto, Yukishige
Tada, Hiroki
Shirakawa, Eiji
Inagaki, Eiji
Shibata, Saizo
Nakamura, Ikuro
Hayashi, Yoshiharu
Ikegami, Kiyoteru
Uchida, Itsuo
A series of renin inhibitors containing the (2S,3S,5S)-2-amino-1- cyclohexyl-6-methyl-3,5-heptanediol (2-amino-3,5-anti-diol) fragment as a novel transition-state mimic was synthesized, and their biological activities were evaluated. All of the synthesized compounds containing the 2-amino-3,5- anti-diol fragment at the P1-P1' position showed high in vitro renin- inhibitory activity with IC50 values in the 10-8-10-10 M range, and most of them caused a reduction of blood pressure when administered orally to salt-depleted, conscious marmosets. The inhibitor (29) with the 4- hydroxypiperidine residue at the P4 position showed the highest activity in terms of both potency and duration of the blood pressure-lowering effect.
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