FIELD: chemistry.
SUBSTANCE: invention relates to oxazolidinone derivative represented by the formula (1):
wherein R is a heterocyclic group selected from the following groups represented by the formula (1a):
(1а),
R1 is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; R2 is hydrogen, C1-C6-alkyl, -CH2-CH = CH2, -CH2-FROMCH,≡ -C(O)CH(OH)CH2OH, -CH2-C(O)OC2H5, -CH2CH2OH, -CH2C(O)OH, -CH2C(O)OC(CH3)3, -C(O)CH2OH, -C(O)CH2OC (O)CH3, or (CH2)mC(=O)R21, where R21 is hydrogen, (CH2)nNHR211, where R211 is hydrogen or C1-C6 alkyl, or CH(OH)CH2OH, and m and n, each independently represent an integer from 0 to 3; and Q is OR3, NHR3 or 1,2,3-triazole, where R3 is hydrogen, C1-C6-alkyl, -C(=O)R31 or a heteroaromatic cyclic group selected from isoxazol-3-yl or isoxazol-5-yl, R31 is hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl or O-(C1-C6) alkyl. The invention also relates to oxazolidinone prodrug represented by a compound selected from compounds of formulas (5)-(7) wherein Q is the same substituents as specified for the compounds of formula (1), and M+ represents an alkali metal ion such as Na or K Or an ammonium ion. Compounds of the invention also relate to specific oxazolidinone derivatives listed in the claims. Compounds of the invention are intended for manufacture of a pharmaceutical composition for antibiotic comprising (a) a therapeutically effective amount of oxazolidinone and (b) a pharmaceutically acceptable carrier, diluent, excipient or combination thereof.
EFFECT: oxazolidinone derivatives with antibiotic activity.
6 cl, 1 tbl, 113 ex
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