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Abstract

Antimicrobial quinolone thiourea compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 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) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and (2) X is --R.sup.15 --N(R.sup.16)(R.sup.17) or --R.sup.15 --R.sup.18 --N(R.sup.19)(R.sup.17), where (a) (1) R.sup.15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R.sup.16 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) when X is R.sup.15 --N(R.sup.16)(R.sup.17), R.sup.16 and R.sup.15 may together comprise a heterocyclic ring including the nitrogen atom to which R.sup.15 and R.sup.16 are bonded; (b) R.sup.17 is C(.dbd.S)--NR.sup.20 R.sup.21 ; where R.sup.20 is, hydrogen, alkyl, alkenyl, a carbocyclic ring or a heterocyclic ring; and R.sup.21 is R.sup.20 or N(R.sup.20)(R.sup.20); or R.sup.20 and R.sup.21, together with the nitrogen to which they are bonded, form a heterocyclic ring; and (c) (1) R.sup.18 is alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R.sup.19 is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) R.sup.18 and R.sup.19 may together comprise a heterocyclic ring including the nitrogen atom to which R.sup.18 and R.sup.19 are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

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First Claim