| 摘要 |
Biotin derivs. of formula (I), opt. (where appropriate) in D- or L-form, and their salts are new, where Q is absent, or is NH-(CH2)n-CO or NH-(CH2)n-NH; R<1> = X-Arg-Gly-Asp-Y, A-Cys(R<2>)-B-U or cyclo-(Arg-Gly-Asp-Z), Z being attached in the side chain of Q or (where Q is absent) to biotin; X, Y = an amino acid residue or a di-, tri-, tetra- or pentapeptide residue, the amino acids being selected from Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, 4-halo-Phe, His, homo-Phe, Ile, Leu, Lys, Met, Nle, Phe, Phg, Pro, Ser, Thr, Trp, Tyr and Val and their derivs.; A is absent, or is Asp or a peptide fragment selected from Ala-Asp, Thr-Ala-Asp, Lys-Thr-Ala-Asp, Lys-Thr-Ala-Asn, Lys-Thr-Gly-Asp, Lys-Ala-Ala-Asp, Arg-Thr-Ala-Asp, Ser-Ala-Asp, Gln-Ser-Ala-Asp, Glp-Ser-Ala-Asp, Gly-Lys-Thr-Ala-Asp, Asn-Gly-Lys-Thr-Ala-Asp, Ile-Ser-Ala-Gly, Arg-Ser-Ala-Gly, Cys-Asn-Gly-Lys-Thr-Ala-Asp, Tyr-Cys-Asn-Gly-Lys-Thr-Ala-Asp, Asp-Tyr-Cys-Asn-Gly-Lys-Thr-Ala-Asp, Asp-Asp-Tyr-Cys-Asn-Gly-Lys-Thr-Ala-Asp, Gly-Lys-Thr-Cys(Trt)-Asp, Met-Asp-Asp-Tyr-Cys-Asn-Gly-Lys-Thr-Ala-Asp or Asp-Met-Asp-Asp-Tyr-Cys-Asn-Gly-Lys-Thr-Ala-Asp; B is (i) absent, (ii) OH, Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, 4-halo-Phe, His, Ile, Leu, Lys, Met, Orn, Phe, Pro, Ser, Thr, Trp, Tyr, Val or an N-methylated deriv. of these, or (iii) a peptide fragment selected from Pro-Arg, Pro-Arg-Asn, Pro-Arg-Asn-Pro, Pro-Arg-Asn-Pro-His, Pro-Arg-Asn-Pro-His-Lys, Pro-Arg-Asn-Pro-His-Lys-Gly, Pro-Arg-Asn-Pro-His-Lys-Gly-Pro, Pro-Arg-Asn-Pro-His-Lys-Gly-Pro-Ala or Pro-Arg-Asn-Pro-His-Lys-Gly-Pro-Ala-Thr; R<2> = H, 1-6C alkyl, Trt, Dpm or Bzl; U = OH, OR<9>, NH2, NHR<9> or N(R<9>)2; Z = an amino acid residue or a di, tri- or tetrapeptide residue, the amino acids being selected from Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val and M and derivs. of these, where the amino acid residues are linked together in peptide fashion via the alpha -amino and alpha -carboxy gps.; provided that an amino acid residue M is always present; M = the residue of an amino acid of formula NH(R<8>)-CH(R<3>)-COOH; R<3> = a gp. -R<5>-R<4>, -R<6>-R<4> or -R<7>-R<4>; R<4> = OH, NH2, SH or COOH; R<5> = 1-6C alkylene; R<6> = 7-14C alkylenephenyl; R<7> = 8-14C alkylenephenylalkylene; R<8> = H, 1-6C alkyl or 7-12C alkylenephenyl; R<9> = 1-6C alkyl; halo = F, Cl, Br or I; n = 1-10; Glp = pyroglutamic acid; Phg = phenylglycine; Trt = trityl; provided that when R<1> is a gp. A-Cys(R<2>)-B-U, then only one of A and B may be absent. |
