| 摘要 |
Peptide derivatives (I) are new. Peptide derivatives of formula R5-A-NH-Y(R1)-V'-U'-Z (I) and their prodrugs and salts are new. A = P2-P1; P1 = a group of formula N(R3)-X(R2)-CO; P2 = a group of formula (i); R1 = H or (CH2)aCOOR6; a = 0-5; R6 = 1-6C alkyl; R2 = H, 1-8C alkyl, (CH2)cCOOR8, (CH2)dOH, (CH2)eQ or (CH2)kOCOOR16; c, d = 1-4; R8 = H or 1-6C alkyl; Q = R10, OR10, SR10, guanidino, imidazolyl or NHR10; e = 1-5; R10 = H, 1-16C alkyl or aryl, heteroaryl, aralkyl or heteroaralkyl (all optionally substituted); k = 1-8; R16 = 1-16C alkyl, or aryl, heteroaryl, aralkyl or heteroaralkyl (all optionally substituted), adamantyl, camphor or cyclohexylmethyl; R3 = (CH2)bR7; b = 1-8; R7 = H, 1-10C alkyl or a charged group; R4 = 1-8C alkyl, (CH2)fOR11, (CH2)fSR11 or (CH2)fNHR11; f = 1-8; R11 = H or COOR17; R17 = 1-16C alkyl, or aryl, heteroaryl, aralkyl or heteroaralkyl (all optionally substituted), adamantyl, camphor or cyclohexylmethyl; R5 = (CH2)g(CH3)h, (CH2)i-aryl, SO2R12, COR12 or COOR12, all optionally modified with a charged or uncharged group; i = 0-3; g + h = 0-3; R12 = 1-16C alkyl, or aryl, heteroaryl, aralkyl or heteroaralkyl (all optionally substituted), adamantyl, camphor or cyclohexylmethyl; U' = phenyl, cyclohexyl, heterophenyl or heterocyclohexyl; V' = (CH2)n; n = 0-3; X = N or CH; Y = N or (CH)m; m = 0 or 1; Z = aminomethyl, guanidino or C(NH)NHR14 in the 3 or 4 position; R14 = H, OH, NH2, COR15 or COOR15, and R15 = 1-16C alkyl or aryl, heteroaryl, aralkyl or heteroaralkyl (all optionally substituted), provided that at least one charged group is in R1, R2, R3 or R5. An Independent claim is also included for preparation of (I).
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