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Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas

[ Vol. 16 , Issue. 5 ]

Author(s):

Sandra Piras, Paola Corona, Roberta Ibba, Federico Riu, Gabriele Murineddu, Giuseppina Sanna, Silvia Madeddu, Ilenia Delogu, Roberta Loddo* and Antonio Carta*   Pages 677 - 688 ( 12 )

Abstract:


Background: Coxsackievirus infections are associated with cases of aseptic meningitis, encephalitis, myocarditis, and some chronic disease.

Methods: A series of benzo[d][1,2,3]triazol-1(2)-yl derivatives (here named benzotriazol-1(2)-yl) (4a-i, 5a-h, 6a-e, g, i, j and 7a-f, h-j) were designed, synthesized and in vitro evaluated for cytotoxicity and antiviral activity against two important human enteroviruses (HEVs) members of the Picornaviridae family [Coxsackievirus B 5 (CVB-5) and Poliovirus 1 (Sb-1)].

Results: Compounds 4c (CC50 >100 μM; EC50 = 9 μM), 5g (CC50 >100 μM; EC50 = 8 μM), and 6a (CC50 >100 μM; EC50 = 10 μM) were found active against CVB-5. With the aim of evaluating the selectivity of action of this class of compounds, a wide spectrum of RNA (positive- and negativesense), double-stranded (dsRNA) or DNA viruses were also assayed. For none of them, significant antiviral activity was determined.

Conclusion: These results point towards a selective activity against CVB-5, an important human pathogen that causes both acute and chronic diseases in infants, young children, and immunocompromised patients.

Keywords:

Benzotriazole derivatives, antiviral activity, enterovirus, coxsackievirus, cytotoxicity, rna virus, picornaviridae.

Affiliation:

Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari, Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari, Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari, Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari, Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari, Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari

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