New tricyclic indolyl-substituted oxazolidinone derivatives, useful as broad spectrum antibacterial agents of low toxicity

摘要

3-(Tricyclic indolyl)-5-(substituted methyl)-2-oxazolidinones (I) are new. Oxazolidinone derivatives of formula (I) and their stereoisomers and salts are new. -U-V- = -CHR3-C(=D)-, -CHR4-CH2-, -CH2-CHR5- or -C(=G)-CH2-; n = 1-3; R2 = H, halo or 1-4C alkyl; E = H or halo; R3, R4 = H; 3-6C cycloalkyl; -COR6; up to 6C acyl (optionally substituted (os) by halo, OH or 1-5C alkoxy); 1-6C alkyl or 2-6C alkenyl (both os by CN, halo, COOH, up to 5C alkoxycarbonyl, OR9 or NR10R11; and/or by 6-14C aryl, itself os by halo, 1-6C alkyl, 1-6C alkoxy or up to 6C acyl); OR12; or NR13R14; D, G = O or S; R5 = OR15 or NR16R17; R6 = H, 1-6C alkoxy or NR7R8; R7 - R17 = H, Ph or 1-5C alkyl; R1 = N3, OR18, OSO2R19 or NHR21; R18 = H, 1-6C alkyl or up to 6C acyl; R19 = 1-6C alkyl or Ph; R21 = -C(=Q)-R22 or -P(O)(OR23)(OR24); Q = O or S; R22 = 1-8C alkyl, 1-8C alkoxy or CF3; 3-6C cycloalkyl (os by halo or 6-10C aryl); 6-10C aryl or 5- or 6-membered saturated or aromatic heterocycle containing 1-3 of S, N and/or O as heteroatoms (both os by 1 or 2 of halo, CN, NO2, OH and Ph); or NR25R26; R25, R26 = H, Ph, pyridyl or 1-5C alkyl (os by morpholino); R23, R24 = H or 1-4C alkyl. An Independent claim is included for the preparation of (I).