Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas
Author:
Piras Sandra1ORCID, Corona Paola1ORCID, Ibba Roberta1ORCID, Riu Federico1ORCID, Murineddu Gabriele1ORCID, Sanna Giuseppina2ORCID, Madeddu Silvia2ORCID, Delogu Ilenia2ORCID, Loddo Roberta2ORCID, Carta Antonio1ORCID
Affiliation:
1. Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23, 07100 Sassari, Italy 2. Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Italy
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.
Funder
MIUR Assessorato della Programmazione, Bilancio, Credito e Assetto del Territorio, della Regione Autonoma della Sardegna
Publisher
Bentham Science Publishers Ltd.
Reference36 articles.
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