| 摘要 |
Peptide analogues of formula (I) and their salts are new where G = SH or OH; L = CH2 or CO; W = H, an N-protecting gp., alkyl, alkenyl, aralkyl, aralkenyl, R3CO, R5R4NCO or R6SO2; R3 = H, CF3, alkoxy, alkyl, mono- or diarylalkyl, mono- or dipyridylalkyl, Ar1, pyridyl, morpholino, piperazinyl, quinolyl N-oxide, pyridyl N-oxide, 1-(2-amino-4-thiazolyl)-1 propenyl or a gp. of formula (a)-(f): Ar1 = aryl opt. substd. by halogen, CF3, OCF3 or alkyl; R7 = phenyl or naphthyl; R8-R10 = alkyl, aralkyl or alkanyl; m = 0-2; T = cyclohexyl; p = 1-3; Y and Y1 = CO or SO2; t = 0 or 1; R11 and R'11 = OH or alkoxy; s = 1 or 2; R4 and R5 = H, aryl, alkaryl, haloaryl, cycloalkyl or alkyl; R6 = alkyl, A, B and D are absent or are gps. of formula (g)-(i): x = 1 or 2; r = 0 or 1; z = 0 or 1; R12 = H or alkyl; R13 = H, cycloalkyl, aryl, or alkyl opt. substd. by SMe, OH, SH, guanidyl, NR14R15, COR16, cycloalkyl, Ar2 or Het; R14 and R15 = H, alkyl or phenyl; R16 = OH, benzyloxy, alkoxy or NR14R15; Ar2 = aryl opt. substd. by OH, halogen, NO2, alkoxy or NR14R15; Het = 5- or 6-membered N-contg. heterocyclyl or indolyl, opt. N-substd. by alkyl or a protecting gp.; R1 = alkyl or alkenyl, opt. substd. by cycloalkyl or Ar3; Ar3 = aryl opt. substd. by halogen, NO2, OH, NH2 or alkoxy; n = 1 or 2; R2 and R'2 = OH or alkoxy. Intermediates of formula (II) are also new, provided that D is not absent. |
