| 摘要 |
<p>Macrocyclic cpds. of formula (I) are new. In (I) R1 is H, in which case R2 is H, and R3 and R4 are both H or both hydroxy, or R1 is hydroxy, in which case R2 is H, R3 is hydroxy or 1-6C alkoxy and R4 is hydroxy, or R2 is aminocarbonyl and then R3 and R4 are both hydroxy; R5 is -W.CO.R6; W is -CO.A.NH-, -CO.CHR7.NH-, or R6 is 1-17C alkyl or 2-17C alkenyl. A is 1-10C alkylene or 5-6C cycloalkylene; R7 is hydroxy- or mercapto- ethyl or -methyl, methylthioethyl, 2-thienyl, 3-indolemethyl or phenyl or benzyl both opt. ring-substd. by chloro, bromo, iodo, nitro, 1-3C alkyl or alkylthio, hydroxy, carbamoyl or 1-3C alkylcarbamoyl; X is H, chloro, bromo, iodo, nitro, 1-3C alkyl, alkoxy or alkylthio, hydroxy, mercapto, carbamoyl or 1-3C alkylcarbamoyl; X1 is chloro, bromo or iodo; One Q is NH, the other is H; B is (CH2)n, CH:CH, CH:CH.CH2 or CO.NH.CH2; and n is 1-3. (I) inhibit the growth of pathogenic fungi both in vivo and in vitro. They are useful for treating infections caused by Trichophyton mentagrophytes and esp. Candida albicans and can be administered orally as well as topically.</p> |
