| 摘要 |
New diamino acid derivatives of the formula I X-Z-NH-CH(CH2R1)-CH(NH2)-CH2-CO-E-G-Y I wherein X is H, R2-O-CnH2n-CO-, R2-CnH2n-O-CO-, R2-C2n-CO-, R2-SO2, (R2-CnH2n)-L(R2-CrH2r)-CtH2t-CO-, H-(NHCH2CH2)n-NH-CH2CO- or 9-fluorenyl-CnH2n-O-CO-, Z is 0 to 4 amino acid radicals, bonded to one another in a peptide-like manner, selected from the group consisting of Abu, Ada, Ala, Arg, Dab, Gly, His, Ile, Leu, tert.-Leu, Lys, Met, Nbg, Nle, N-Me-His, N-Me-Phe, Orn, Phe, Pro, Ser, Thr, Tic, Trp, Tyr and Val, R1 is H, A, cycloalkyl with 3-7 C atoms, Ar or CpH2p-W, E is absent or is Ala, Gly, Ile, Leu, tert.-Leu, Met, Ser, Thr or Val, G is absent or is His, Phe, Trp, Tyr or -NH-CH(CH2R1)-CH(NH2)-CH2CO-, Y is -O-CmH2m-R3, -NH-CmH2m-R3, -NH-CmH2m-1(R3)2 or NA2, R2 is A, cycloalkyl with 3-7 C atoms, benzyl or Ar, L is CH or N, R3 is H, A, cycloalkyl with 3-7 C atoms, Ar, pyridyl, imidazolyl, piperidyl, N-benzyl-piperidyl or piperazinyl, W is OH, NH2, OA, NHA or NA2, A is alkyl with 1-6 C atoms, Ar is unsubstituted phenyl, phenyl which is mono- or poly-substituted by A, AO, F, Cl, Br, I, CF3 and/or NH2, or unsubstituted naphthyl and m, n, p, r and t are each 0, 1, 2, 3, 4 or 5, and salts thereof, inhibit the activity of human plasma renin. |
