Anti-HIV activity of new substituted 1,3,4-oxadiazole derivatives and their acyclic nucleoside analogues.

نویسندگان

  • Wael A El-Sayed
  • Farag A El-Essawy
  • Omar M Ali
  • Barsis S Nasr
  • Mohamed M Abdalla
  • Adel A-H Abdel-Rahman
چکیده

A number of new 5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazole derivatives, 2-5 and 8-11, were synthesized. The 2-{5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazol-2-ylthio}acetohydrazones 6a and 6b were synthesized by the reaction of the hydrazide 4 with the corresponding monosaccharides. Cyclization of the sugar hydrazones 6a and 6b with acetic anhydride afforded the substituted oxadiazoline derivatives 7a and 7b. The synthesized compounds were evaluated for their antiviral activity against, the human immunodeficiency virus (HIV-1) and some of these compounds showed moderate to high antiviral activity.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Novel Oxadiazole Thioglycosides as Potential Anti- Acinetobacter Agents

The glycosylation of 1,3,4-oxadiazole-2-thiones has been performed with peracetylated β-pyranosyl bromide in the presence of potassium carbonate. Deprotection of acetylated thioglycosides was necessary for increasing their antibacterial effects. The structure of nucleosides were confirmed by 1H NMR, 13C NMR and HRMS. The anomeric protons of nucleosides c1–4 were assigned to the doublet, confirm...

متن کامل

Novel Oxadiazole Thioglycosides as Potential Anti- Acinetobacter Agents

The glycosylation of 1,3,4-oxadiazole-2-thiones has been performed with peracetylated β-pyranosyl bromide in the presence of potassium carbonate. Deprotection of acetylated thioglycosides was necessary for increasing their antibacterial effects. The structure of nucleosides were confirmed by 1H NMR, 13C NMR and HRMS. The anomeric protons of nucleosides c1–4 were assigned to the doublet, confirm...

متن کامل

Synthesis, Characterization and Anti-Inflammatory Activity of Some 1, 3,4 -Oxadiazole Derivatives

A series of five-membered heterocyclic rings were synthesized by the reaction between benzoyl chloride and various chlolro-nitro-benzoyl chlorides and semi carbazide to form (C1-C7) compounds and was tested for their anti-inflammatory activity determined by rat-paw-oedema method. All the synthesis compounds have been characterized by 1HNMR, IR and Mass spectral data. The compounds were purified...

متن کامل

Syntheses of Substituted 1,3,4-Oxadiazole, 1,3,4-Thiadiazole and 1,2,4-Triazole Derivatives as Potential Antimicrobial Agents

A series of 2-(4-nitro-1-imidazolylmethyl)-1,3,4-oxadiazole, 1,3,4-triazole and 3-(4-nitro-1-imidazolylmethyl)-1,2,4-triazole derivatives were synthesized and tested for their antimicrobial activity. Some of the tested compounds were active against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Clostridium difficile, Aspergillus niger and Cryptococcus neoformans.

متن کامل

One-pot, four-component synthesis of fully substituted 1,3,4-oxadiazole derivatives from N-isocyaniminotriphenylphosphorane (Ph3PNNC), a primary amine, a carboxylic acid and cinnamaldehyde

The imine intermediate generated by the addition of primary amine to the cinnamaldehyde is trapped by the N-isocyaniminotriphenylphosphorane (Ph3PNNC) and a carboxylic acid, and leads to the formation of the corresponding iminophosphorane intermediate. The 1,3,4-oxadiazole derivatives are formed via intramolecular aza-Wittig reaction of the iminophosphorane intermediate. The reactions were comp...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Zeitschrift fur Naturforschung. C, Journal of biosciences

دوره 64 11-12  شماره 

صفحات  -

تاریخ انتشار 2009