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Merck
  • Synthesis of novel sulfanilamide-derived 1,2,3-triazoles and their evaluation for antibacterial and antifungal activities.

Synthesis of novel sulfanilamide-derived 1,2,3-triazoles and their evaluation for antibacterial and antifungal activities.

European journal of medicinal chemistry (2010-08-17)
Xian-Long Wang, Kun Wan, Cheng-He Zhou
摘要

A series of novel sulfanilamide-derived 1,2,3-triazole compounds were synthesized in excellent yields via 1,3-dipolar cycloaddition and confirmed by MS, IR and NMR spectra as well as elemental analyses. All the compounds were screened in vitro for their antibacterial and antifungal activities. Preliminary results indicated that some target compounds exhibited promising antibacterial potency. Especially, 4-amino-N-((1-dodecyl-1H-1,2,3-triazol-4-yl)methyl) benzenesulfonamide, N-((1-(2,4-dichlorobenzyl)- 1H-1,2,3-triazol-4-yl)methyl)-4-aminobenzenesulfonamide and 4-amino-N-((1-(2,4-difluorobenzyl)- 1H-1,2,3-triazol-4-yl)methyl) benzenesulfonamide were found to be the most potent compounds against all the tested strains except for Candida albicans (ATCC76615) and Candida mycoderma.

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Sigma-Aldrich
对氨基苯磺酰胺, ≥98%
Supelco
磺胺熔点标准品, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
对氨基苯磺酰胺, puriss. p.a., ≥98% (calc. to the dried substance)
Supelco
对氨基苯磺酰胺, VETRANAL®, analytical standard