| 摘要 |
<p>Tylosin derivs. of formula (I) are new. (R1 is OH, halogen, NR5R6, NX (opt. substd. by an oxo gp., OH, 1-6C alkyl or 1-6C hydroxyalkyl), or imidazolyl, morpholino or piperazino (each opt. substd. by 1-6C alkyl) or O-COCH2R8; R5 is H or 1-6C alkyl opt. substd. by a OH gp.; R6 is H, 1-6C alkyl opt. substd. by a OH gp., aryl, aralkyl, 3-10C cycloalkyl, CO(O)mR7 or CH2R13; m is 0 or 1; R7 is 1-6C alkyl, aryl, aralkyl, furaryl or pyridinyl; R13 is CH2F, CHF2 or CF3; X is (CH2)n; n is 2-15; R8 is NR9R10 or SR11; R9 and R10 are H or 1-6C alkyl; or R9 + R10 form 3-7C alkylene; R11 is furanyl or pyridinyl; R2 is H or 1-6C alkanoyl; R3 is Me or CH2CHO; R4 is H or OH; A is O, (alpha H, beta OH) or (alpha OH, beta H); the wavy line is a single or double bond; and the broken line is a single or double bond or an epoxy-bridged single bond. Provided that (1) when R1 is OH, R3 is Me and R4 is H, or the broken line is an epoxy-bridged single bond; and (2) when R1 is halogen, R3 is Me or the broken line is an epoxy-bridged bond). (I) are broad-spectrum antibacterials with greater activity then tylosin. Dose is 0.01-1 g administered 1-4 times daily.</p> |
