摘要 |
Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of formula (III), preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z5 is alpha -H; one Z7 is beta -H and the other is alpha -H or alpha -OH; both substituents Z12 are hydrogen; X' is a polyamine side chain of the formula -NH-(CH2)p-NH-(CH2)q-N(R<II>)(R<III>) where p and q are each independently 3 or 4, and R<II> and R<III> are each independently hydrogen or methyl; R' is methyl; and Y' is (C1-C10)-alkyl substituted with a group such as -CO2H or -SO3H. Such compounds, as well as squalamine itself, have antiangiogenic activity and Na<+>/K<+>-ATPase-inhibiting activity.
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申请人 |
MAGAININ PHARMACEUTICALS INC.;FRYE, LEAH, L.;ZASLOFF, MICHAEL, A.;KINNEY, WILLIAM, A.;MORIARTY, ROBERT;COLLINS, DELWOOD, C. |
发明人 |
FRYE, LEAH, L.;ZASLOFF, MICHAEL, A.;KINNEY, WILLIAM, A.;MORIARTY, ROBERT;COLLINS, DELWOOD, C. |