| 摘要 |
Antimicrobial quinolone thiourea compounds of the general formula: <IMAGE> wherein (1) A1, 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 R1 and R3 are X; and (2) X is -R15-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 R15-N(R16)(R17), R16 and R15 may together comprise a heterocyclic ring including the nitrogen atom to which R15 and R16 are bonded; (b) R17 is C(=S)-NR20R21; where R20 is, hydrogen, alkyl, alkenyl, a carbocyclic ring or a heterocyclic ring; and R21 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) R18 and R19 may together comprise a heterocyclic ring including the nitrogen atom to which R18 and R19 are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.
|
