Novel antimicrobial quinolone thioureas

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) C07D 215/56 (2006.01) C07D 401/12 (2006.01) C07D 405/04 (2006.01) C07D 409/04 (2006.01) C07D 417/04 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2077435

2077435 9116310 PCTABS00007 Antimicrobial quinolone thiourea compounds of general formula (I), 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.

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