NOVEL INHIBITORS OF MONO- AND BICYCLO HYRASE

FIELD: pharmacology, medicine. SUBSTANCE: desired compounds being mono- and bicyclo compounds have formulawhere Xis -S- or -SO-; Ris hydrogen, halogen or lower alkyl being optionally substituted by halogen; Ris hydrogen, hydroxy, amino, lower alkyl amino, di-lower alkyl amino being optionally substituted by lower alkoxy or by -OP group which is easily hydrolyzed; Ris hydrogen, hydroxy, lower alkyl, halogen or by -OP group; Ris hydrogen, hydroxy or by -OP group; Ris hydrogen, cyano, optionally substituted by esterifized carboxy or optionally substituted amidated (thio)carboxy, optionally substituted by alkyl, optionally substituted alkenyl or optionally substituted heterocycle; Ris NR-A, -N=B or optionally substituted heterocycle where Ris hydrogen or lower alkyl, A is optionally substituted iminoyl, optionally substituted (thio)acyl, optionally substituted esterifized carboxy, optionally substituted carboxy, optionally substituted amidated (thio)carboxy or optionally substituted heterocycle and B is optionally substituted alkylydene; Ris cyano, optionally substituted esterifized carboxy or optionally substituted heterocycle, or where Rand Rtogether form -CO-O-Q-X-N(R)- group, and Ris as it mentioned above, Xis (thio)carbonyl or heterocycle, Q is -CH(R)- or -CH(R)-W-; Ris hydrogen or optionally substituted lower alkyl and W is optionally substituted mono-, di-, tri-, tetra- or pentamethylene, proviso that if W is monomethylene, then Xhas value different of (thio)carbonile. Monocyclic compounds having formulawhere substituents are as it mentioned and Rand Rhave separate values, together with bicyclic compounds having formulawhere substituents are mentioned above also are proposed. Said compounds and their pharamaceutically acceptable salts have high antibactericidal activity. EFFECT: improves quality of desired product. Изобретение относится к моно- или бициклическим соединениям общей формулы, указанной в описании, и фармацевтически приемлемым солям моноили бициклических соединений формулы I, обладающих кислотным и/или основным заместителем. Изобретение включает моноциклические соединения общей формулы IA, и бициклические соединения общей формулы IB. Формулы IA и IB также приведены в описании. Эти соединения формулы I, а также их соответствующие фармацевтически приемлемые соли ингибируют активность ДНК-гиразы в бактериях и обладают антибитической, прежде всего антибактериальной активностью в отношении микроорганизмов и могут быть использованы для подавления