| 摘要 |
<p>Antimicrobial quinolone thiourea compounds of general formula (I), wherein (1) A?1, A2, A3, R1, R3, R4, and R6¿ form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and (2) (1) R1 is X, R3 is X, or both R?1 and R3¿ are X; and (2) X is -R?15-N(R16)(R17) or -R15-R18-N(R19)(R17¿), where (a) (1) R15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R16 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) when X is R?15-N(R16)(R17), R16 and R15¿ may together comprise a heterocyclic ring including the nitrogen atom to which R?15 and R16¿ are bonded; (b) R17 is C(=S)-NR20R21; where R20 is hydrogen, alkyl, alkenyl, a carbocyclic ring or a heterocyclic ring; and R?21 is R20 or N(R20)(R20); or R20 and R21¿, together with the nitrogen to which they are bonded, form a heterocyclic ring; and (c) (1) R18) is alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R19 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) R?18 and R19¿ may together comprise a heterocyclic ring including the nitrogen atom to which R?18 and R19¿ are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.</p> |
