New oxazolidinone derivatives useful as antimicrobial agents against Gram-positive and some Gram-negative bacteria, mycobacteria, etc.

摘要

3-Heterocyclyl-5-(substituted methyl)-2-oxazolidinone derivatives (I) are new. 3-Heterocyclyl-5-(substituted methyl)-2-oxazolidinone derivatives of formula (I) and their stereosiomers and salts are new: A = a bi- or tricyclic heterocyclic group of formula (i), (ii) or (iii): D, D', D = H, COOH, halogen, CN, CHO, CF3, NO2 or 1-6C alkoxy, alkoxycarbonyl, alkylthio, acyl or alkyl; E, E' = CH2, O, S, SO or SO2; L = O, S or NR13; R<13> = H, phenyl, OH or 1-6C alkoxy; R<2>-R<5>, R<7>-R<10> = H, or 1-6C alkyl or 2-6C alkenyl optionally substituted by Ar<1>; or R<2>+R<3>, R<4>+R<5>, R<7>+R<8> and/or R<9>+R<10> = O, CH2 or CHR<14>; Ar<1> = 6-10C aryl or 5- or 6-membered heteroaryl (containing 1-3 heteroatoms selected from S, N and O) optionally substituted by 1-6C alkoxy, 1-6C alkyl, OH or halogen; R<14> = 6-10C aryl or 5- to 7-membered heteroaryl (containing 1-3 heteroatoms selected from S, N and O) optionally substituted by 1-6C alkoxy, 1-6C alkyl, OH or halogen; R<6>, R<11>, R<12> = H, 1-6C alkyl, 2-6C alkoxycarbonyl or COR<15>; R<15> = 6-10C aryl, 5- to 7-membered heteroaryl (containing 1-3 heteroatoms selected from S, N and O), 1-4C alkyl or (6-10C)aryl(1-4C)alkyl, where (hetero)aryl is optionally substituted by halogen, CF3, NO2, OH, 1-6C alkyl and/or 1-6C alkoxy; R<1> = N3, OR<16>, OSO2R<17> or NHR<19>; R<16> = H or 1-6C acyl; R<17> = 1-6C alkyl or phenyl; R<19> = H, C(Q)R<20> or P(O)(OR<21>)(OR<22>); Q = O or S; R<20> = 1-8C alkoxy or CF3; 3-6C cycloalkyl optionally substituted by halogen or 6-10C aryl; 6-10C aryl or 5- or 6-membered heterocyclyl (containing 1-3 heteroatoms selected from S, N and O) optionally substituted by 1-2 of halogen, CN, NO2, OH and phenyl; 1-6C alkyl optionally substituted by phenoxy, benzyloxy, COOH, halogen 2-6C alkoxycarbonyl, 1-6C acyl or 5- or 6-membered S-, N- and/or O-containing heterocyclyl; or NR<23>R<24>; R<23>, R<24> = H, phenyl, pyridyl, 1-5C alkyl or morpholino(1-5C)alkyl; R<21>, R<22> = H or 1-4C alkyl.