Bioorganic and Medicinal Chemistry Letters p. 1863 - 1868 (1997)
Update date:2022-08-03
Topics:
Yamada, Yasuki
Ando, Koji
Komiyama, Kazuya
Shibata, Saizo
Nakamura, Ikuro
Hayashi, Yoshiharu
Ikegami, Kiyoteru
Uchida, Itsuo
A series of low molecular renin inhibitors (molecular weight < 600) were prepared and their biological activities were evaluated. The inhibitors containing indole-2-carbonyl moieties at the P3 position and 2-amino-3,5-anti-diol fragment at the P1-P1' position showed renin inhibitory activities with IC50 of 10-8 M order and good blood pressure lowering effects after oral administration to sodium-depleted marmosets.
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