Aims and Scope

The Open Medicinal Chemistry Journal, a peer-reviewed journal, is an important and reliable source of current information on developments in the field. The emphasis is on publishing quality papers and making them freely available to researchers worldwide.


The journal covers all areas of medicinal chemistry, including biological evaluation of novel biologically active compounds, diagnostic agents, or labeled ligands, chemical and analytical techniques used in rational drug design, synthetic chemistry, bioorganic chemistry of small molecules and naturally occurring compounds, structural characterization, pharmacokinetics, and metabolic transformation, toxicology of bioactive compounds including design, synthesis, and evaluation of novel types of prodrugs, quantitative structure-activity relationships, modelling studies, docking studies, new and emerging drug targets, pharmacogenomics, high-throughput screening, and combinatorial chemistry.


Editor's Choice

Antiviral Activity of Benzotriazole Based Derivatives

Paola Corona, Sandra Piras, Roberta Ibba, Federico Riu, Gabriele Murineddu, Giuseppina Sanna, Silvia Madeddu, Ilenia Delogu, Roberta Loddo, Antonio Carta

Background:

For the last thirty years, the benzotriazole scaffold has been the object of our group interest and we have already presented some results on the antiviral activity of our compounds.

Objective:

In this article, we conclude the exploration of N-(4-(R-2H-benzo[d][1,2,3]triazol-2-yl)phenyl)-4-R’-benzamides and 1-(4-(R-2H-benzo[d][1,2,3]triazol-2-yl)phenyl)-3-R’-ureas by synthesizing further modified derivatives, in order to have more elements for SARs evaluation.

Methods:

Here, we reported the synthesis and the antiviral screening results of 38 newly synthesized benzotriazole derivatives against a panel of DNA and RNA viruses. We also analyse SARs in comparing these compounds with previously published benzotriazole analogues, taking stock of the situation.

Results:

Among the newly presented derivatives, compounds 17 and 18 were the most active with EC50 6.9 and 5.5 µM, respectively against Coxsackievirus B5 (CV-B5) and 20.5 and 17.5 µM against Poliovirus (Sb-1).

Conclusion:

we can conclude that N-(4-(2H-benzo[d] [1 - 3] triazol-2-yl)phenyl-R-amide is a good chemical scaffold for the development of new antiviral molecules.


October 23, 2020
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