Some 1,2,4-triazole derivatives: Synthesis and Antiviral Evaluation

Aymn E. Rashad; Ahmed H. Shamroukh; Abeer H. El-Sayed; Jehane A. Micky; Nermin A. Marsok; Farouk M. E. Abdel-Megeid

Abstract

Some 1,2,4-triazole derivatives: Synthesis and Antiviral Evaluation

Author(s): Aymn E. Rashad, Ahmed H. Shamroukh, Abeer H. El-Sayed, Jehane A. Micky, Nermin A. Marsok and Farouk M. E. Abdel-Megeid

The starting material 2-(5-phenyl-3H-1,2,4-triazol-3-ylsulfanyl)acetohydrazide (1) was used as a precursor for preparation of some novel substituted 1,2,4-triazole derivatives 2-6. Also, some acyclic C-nucleosides 7a,e were prepared by treating compound 1 with some aldoses. Moreover, treatment of compound 7b with acetic anhydride gave the acetylated product 8b. Antiviral bioassays were carried out to test compounds 2–5, 7a, 7b, 7d, 7e, and 8b. The CC50 and IC50 were determined in addition to the selectivity index (SI) for tested compounds (Tables 1-3). It was obvious that, most of the tested compounds have significant antiviral activity among of these compounds the sugar hydrazone derivatives 7a, 7b and 7d have the highest antiviral activity against HBV virus in comparing with the antiâ�?influenza drug Zanamivir. While, all of the tested compounds have no antiviral activity against herpetic viral type -1 and type-2 in comparison with reference antiviral drug Acyclovir.

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