摘要 |
<p>Compounds of the formula above, wherein E is H or OH, Q is H or alkyl, R is aryl, alkyl or cycloalkyl substituted with R1, R2 and R3, R1 is H, COOH, COO-alkyl or aryl, R2 is H, alkyl, cycloalkyl or heteroaryl, R3 is H, aryl, OH, alkoxy or optionally protected amino, or Q and R together with the N atom to which they are attached, are COOH or COO-alkyl substituted pyrrolidino, piperidino or 1,2,3,4-tetrahydroisoquinolin-3-yl, three of X1-X4 are independently selected from C(Ra), C(Rb) and C(R3) and the forth X radical is C(R4) or N, Ra-Rd are H, OH, NO2, dialkylamino, halogen, alkyl, alkoxy, aryloxy, aralkyloxy, heteroaralkyloxy, heterocyclylalkyloxy, COOH, COO-alkyl, NH-SO2-alkyl, NHSO2-aryl, NHCO-alkyl, NHCO-aryl, NHCOO-alkyl, NHCO-alkyl-NH2, NHCO-alkyl-NH-G, aralkyl-CONH, alkyl-O-alkyl-CONH, alkyl-COOH, alkyl-COO-alkyl, O-alkyl-COOH or O-alkyl-COO-alkyl, or two adjacent groups of Ra-Rd are alkylenedioxy, G is an amino protecting group, one of G1 & G2 is H and the other is H, alkyl, OH, alkoxy, aroyl, alkanoyl, OCH2, aroyl-OCH2 or a group COO-Rg or OCO-Rg, Rg is halogen, OH, alkoxy, COOH or COO-alkyl substituted alkyl</p> |