New Renin Inhibitors Containing Pseudodipeptidic Units in P_3-P_2 and P_1-P_1' Positions

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概要

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• A series of four non-peptidic renin inhibitors have been designed and synthesized. All of them contain in their molecule (3S, 4S)-4-amino-5-cyclohexyl-3-hydroxypentanoic acid (ACHPA), a hydrophobic portion at the C-terminus and a second dipeptide-like transition state analog or unnatural dipeptidic fragment at the N-terminus. Inhibitory activity of the compounds was measured in vitro by high performance liquid chromatography (HPLC). Their IC_<50> (M/l) values were : <10^<-3> (12), 1.0×10^<-6> (19), 4.0×10^<-4> (23) and 1.0×10^<-6> (29), respectively. All the compounds are stable against chymotrypsin.

• 2005-10-01

著者

• Roman Iza

  National Institute Of Public Health

• PARUSZEWSKI Ryszard

  Department of Drug Chemistry, Medical University

• JAWORSKI Pawel

  Department of Drug Chemistry, Medical University

• BODNAR Magdalena

  Department of Drug Chemistry, Medical University

• DUDKIEWICZ WILCZYNSKA

  National Institute of Public Health

• Jaworski Pawel

  Department Of Drug Chemistry Medical University

• Bodnar Magdalena

  Department Of Drug Chemistry Medical University

• Paruszewski Ryszard

  Department Of Drug Chemistry Medical University

関連論文

• New Renin Inhibitors Containing Pseudodipeptidic Units in P_3-P_2 and P_1-P_1' Positions
• New Renin Inhibitors with Pseudodipeptidic Units in P_1-P_ and P_-P_ Positions
• Amino Acid Derivatives with Anticonvulsant Activity

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