Synthesis of linezolid-like molecules and evaluation of their antimicrobial activities

摘要

3-Fluoro-4-(morpholin-4-yl)aniline (2), prepared from3,4-difluoronitrobenzene, was converted to the corresponding Schiffbase (3) by treatment with indol-3-carbaldehyde. The treatment ofthiourea 4 and carbothioamide derivatives 9 with ethyl bromoacetate or4-substituted phenacyl bromides generated the correspondingthiazolidinone (5 and 13) and thiazoline (6 and 12) derivatives,respectively. The acidic or basic treatment of carbothioamide 9produced 1,3,4-thiadiazole (11) or 1,2,4-triazole (10) compounds,respectively. The structural assignments of the new compounds werebased on elemental analysis and spectral (IR, ^1H-NMR, ^{13}C-NMR, andLC-MS) data. The antimicrobial activity study revealed that allcompounds showed good antitubercular activities.