| 摘要 |
<p>The present invention provides compounds with anti-fungal activity useful for treatment or prevention of fungal infections in human beings or plants. The antifungal compounds are inhibitors of glucan synthase and have the formula (I) (I) wherein Z denotes a mono- or bicyclic aromatic or heteroaromatic ring system; and X1 and X3 are individually selected from the group consisting of -CH and N, wherein at least one of X1 and X3 is N; and X2 is selected from the group consisting of–CH2, -CH-R8 and–(C=O), wherein R8 is C1-3 alkyl; and Y is selected from the group consisting of–(CH2)n-, -(CHR9)-, -(CH2)p-CR10R11- (CH2)q, -(CH2)p-(C=O)-(CH2)q and -(CH2)p-(C=O)-(CH2)q, wherein n is an integer in the range of 1 to 6, p is an integer in the range of 0 to 3 and q is an integer in the range of 1 to 4 and wherein R9 R10 and R11 individually are selected from the group consisting of C1-3-alkyl; and R1 and R5 are individually selected from the group consisting of–H and halogen, wherein at least one of R1 and R5 is halogen; and R2 and R4 is selected from the group consisting of–H and halogen; and R3 is–NH-R6, wherein R6 is selected from the group consisting of–H, alkyl, - (C=O)-R7, -(C=O)-O-R7, - (C=O)-NH2 and–SO2-R7, wherein R7 is selected from the group consisting of–H and alkyl, or a pharmaceutically acceptable salt thereof or a prodrug thereof.</p> |
