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ChemInform Abstract: Novel Renin Inhibitors Containing (2S,3S,5S)-2-Amino-1-cyclohexyl-6-methyl-3,5-heptanediol Fragment as a Transition-State Mimic at the P1—P1′ Cleavage Site.

✍ Scribed by I. UCHIDA; ET AL. ET AL.


Publisher
John Wiley and Sons
Year
2010
Weight
34 KB
Volume
29
Category
Article
ISSN
0931-7597

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✦ Synopsis


Novel Renin Inhibitors Containing (2S,3S,5S)-2-Amino-1-cyclohexyl-6-methyl-3,5-heptanediol Fragment as a Transition-State Mimic at the P1-P1' Cleavage Site.

-A large variety of title compounds (18 examples) are prepared following the sequence shown for (VIa). All compounds containing the 2-amino-3,5-anti-diol fragment exhibit high renin inhibitory effects. Derivative (VIb) shows the highest activity in terms of both potency and duration of the blood pressure lowering effect. -(UCHIDA, I.