| 摘要 |
Peptides of formula (I) and nontoxic salts were prepd.; where X=H or C1-7 acyl; R1= dehydro-pro, D=pGlu, (A)D-Phe, (B)D-Trp, Pro or beta- D-Nal; A=H, Cl, F, NO2, Me, OMe, Cl2 or Br; B=H, NO2, NH2, OMe, F, Cl, Br, Me, NinFor or NinAc; R3= D-Pal, beta-D-Nal or (B)D-Trp; R4= Cys, Asp, Gln, Orn, daB, daP or aBu; R5= Tyr, (c) Arg, (A)Phe, (31) Tyr or His; R6; R6= beta-D-Nal, (B)D-Trp, (A')DPhe, (D)D-Lys, (D)D- Orn, D-Har, D-Tyr, (E)D-His, D-Pal or (C)D-Arg; A'= A, NH2, NHMe or guanidino; C= (lower alkyl)n; n=0, 1 or 2; D= X or aryl; E=H, imBzl or dinitrophenyl. (I) are GnRH analogues with GnRH antagonist activity and are useful for inhibition of prodn. of gonadotropins.
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