- 作者: Abdelal, Ali M. ; El-Emam, Ali A. ; Moustafa, M.A.
- 作者服務機構: Dept. of Medicinal Chemistry, Univ. of Mansoura, Mansoura, Egypt
- 中文摘要: Reaction of 2-trifluoromethyl- or 2-cyanonaphth.lbrak.2,3-d.rbrak. imidazole with 1-O-acetyl-2,3,5-tri-O-benzoyl-.beta.-D-ribofuranose, using the triflate or fusion method afforded 2-trifluoromethyl-1-(2,3,5-tri-O-benzoyl-.alpha.-D- or-.beta.-D- ribofuranosyl)naphth.lbrak.2,3-d.rbrak.imidazole(4 or 6) and 2-cyano-1-(2,3,5-tri-O-benzoyl-.alpha.-D- or.beta.-D-ribofuranosyl)naphth.lbrak.2,3-d.rbrak.imidazole(5 or 7), respectively. The products 4 and 5 or 6 and 7 were separated by chromatography on silica gel. Treatment of the blocked nucleosides 4-7 with methanolic NH/sub 3/ at 0.degree.C furnished the deblocked nucleosides 8-11 respectively. Treatment of 10 with 5% NH/sub 3/ (aq) at 60.degree.C gave 11. Structural elucidation is based on elemental analysis, UV, FAB-MS and /sup 1/H NMR spectra. Compounds 4-11 were subjected to antibacterial testing. Compounds 5, 7 and 10 have significant activity against Staphylococcus aureus(gram positive) and Escherichia coli (gram negative) bacteria, whereas the other tested compounds showed no significant activity.
- 英文摘要: --
- 中文關鍵字: Antibacterial Agent (Antibacterial Drug); Naphthimidazole Ribonucleoside
- 英文關鍵字: 抗菌劑