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Matches in SemOpenAlex for { <https://semopenalex.org/work/W1995478204> ?p ?o ?g. }

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• W1995478204 abstract "A series of transition-state analogues having heterocyclythio C-termini has been synthesized and evaluated for inhibition of human renin. Addition of mercaptoheterocycles to a chiral Boc-amino epoxide intermediate led, after several steps, to the target [(2R,3S)-3-(BocPheHis-amino)-4-cyclohexyl-2-hydroxy-1-butyl]thio derivatives. Oxidation of the thioether to sulfone was also investigated. Several of the compounds, especially those derived from N1-substituted-5-mercaptotetrazoles or N4-substituted-3-mercapto-5-(trifluoromethyl)-1,2,4-triazoles, were moderately potent inhibitors of human plasma renin, having IC50 values of 30-40 nM. When selected compounds were administered intravenously to sodium-deficient rhesus monkeys at 0.3-1.2 mg/kg, they reduced plasma renin activity by 75-98%. However, this inhibition and the accompanying drop in blood pressure were of short duration." @default.
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• W1995478204 date "1992-05-01" @default.
• W1995478204 modified "2023-10-16" @default.
• W1995478204 title "Renin inhibitors containing C-termini derived from mercaptoheterocycles" @default.
• W1995478204 doi "https://doi.org/10.1021/jm00089a023" @default.
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