Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 24, Issue 10, Pages 3660-3670Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-015-1410-0
Keywords
Fluorinated benzothiazole derivates; Substituted benzoyl chloride; Antimicrobial activity; Antifungal activity
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A series of novel 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-substituted phenyl amides was synthesized by the condensation reaction of (1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethanamine with substituted benzoyl chlorides under mild conditions. Their structures were confirmed by H-1 NMR, C-13 NMR and F-19 NMR spectra, elemental analyses and in three cases also by single-crystal X-ray diffraction techniques. The optical activities were confirmed by optical rotation measurements. All the synthesized compounds were screened for antibacterial and antifungal activity against a variety of bacterial and fungal strains. Some of the compounds reveal antibacterial and antifungal activity comparable or slightly better to that of chloramphenicol, cefoperazone and amphotericin B used as medicinal standards.
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