New renin inhibitors containing pseudodipeptidic units in P3-P2 and P1-P1' positions |
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Authors: | Paruszewski Ryszard Jaworski Paweł Bodnar Magdalena Dudkiewicz-Wilczyńska Jadwiga Roman Iza |
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Institution: | Department of Drug Chemistry, Medical University, Poland. rpbw@farm.amwaw.edu.pl |
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Abstract: | 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 IC50 (M/l) values were: <10(-3) (12), 1.0 x 10(-6) (19), 4.0 x 10(-4) (23) and 1.0 x 10(-6) (29), respectively. All the compounds are stable against chymotrypsin. |
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