发明公开
EP0366643A2 Novel antimicrobial dithiocarbamoyl quinolones 失效
Antimikrobielle二硫代氨基甲酰喹诺酮。

Novel antimicrobial dithiocarbamoyl quinolones
摘要:
Antimicrobial dithiocarbamoyl quinolone compounds of the general formula:
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)-S-M, where M is a pharmaceutically-­acceptable salt or biohydrolyzable ester; 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.
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