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    • 6. 发明授权
    • Derivatives of A54145 cyclic peptides
    • A54145环肽衍生物
    • US5028590A
    • 1991-07-02
    • US179929
    • 1988-04-11
    • David S. FukudaJon S. Mynderse
    • David S. FukudaJon S. Mynderse
    • A61K38/00C07K7/08
    • C12R1/54C07K7/08A61K38/00Y02P20/55
    • A new group of cyclic peptide derivatives, the A54145 cyclic peptide derivatives, which have the general formula: ##STR1## wherein: R is C.sub.8 -C.sub.18 -alkyl, optionally substituted C.sub.8 -C.sub.18 -alkanoyl or C.sub.8 -C.sub.18 -alkenoyl;(R,R.sup.2)-Trp represents a group of formula ##STR2## (Lys-R.sup.1) represents --NH(CH.sub.2).sub.4 CH(NHR.sup.1)CO--; R.sup.1 is hydrogen or an amino-protecting group; andR.sup.2 is hydrogen; orR and R.sup.2, taken together, represent a C.sub.8 -C.sub.18 -alkylidene group;X is Ile or Val; andY is Glu or 3-MG;provided that: 1) when R.sup.1 =H, X=Ile and Y=Glu or 3-MG, R cannot be 8-methylnonanoyl, 8-methyldecanoyl or n-decanoyl; 2) when R.sup.1 =H, X=Val and Y=3-MG, R cannot be 8-methyldecanoyl; and 3) when R.sup.1 =H, X=Val and Y=Glu, R cannot be 8-methylnonanoyl; and 4) when R.sup.1 is an amino protecting group, R cannot be 8-methylnonanoyl, 8-methyldecanoyl, or n-decanoyl; and their salts are antibacterial agents or intermediates to such agents. Formula 1 compounds wherein R.sup.2 is hydrogen improve growth perforamnce in animals; thus, feed compositions for promoting growth in animals such as poultry and methods for increasing growth in animals using these compositions, are also provided.
    • 具有以下通式的新一组环肽衍生物A54145环肽衍生物:(R,R 2)TrpGlu(HO)Asn 1 + TR< IMAGE>其中:R为C 8 -C 18烷基,任选取代的C 8 - C18-烷酰基或C8-C18-烯酰基; (R,R 2)-Trp表示式(A 1-R 1)表示-NH(CH 2)4 CH(NHR 1)CO-的基团。 R1是氢或氨基保护基; R2是氢; 或R 1和R 2一起代表C 8 -C 18亚烷基; X是Ile或Val; Y为Glu或3-MG; 条件是:1)当R1 = H,X = Ile,Y = Glu或3-MG时,R不能是8-甲基壬酰基,8-甲基癸酰基或正癸酰基; 2)当R1 = H,X = Val和Y = 3-MG时,R不能是8-甲基癸酰基; 和3)当R1 = H,X = Val和Y = Glu时,R不能是8-甲基壬酰基; 和4)当R 1是氨基保护基时,R不能是8-甲基壬酰基,8-甲基癸酰基或正癸酰基; 并且它们的盐是这种试剂的抗菌剂或中间体。 其中R2是氢的式1化合物改善动物中的生长穿孔; 因此,还提供了用于促进动物如家禽生长的饲料组合物和使用这些组合物增加动物生长的方法。