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

Preliminary anti-coxsackie activity of novel 1-[4-(5,6-dimethyl(h)1h(2h)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas / Piras, S.; Corona, P.; Ibba, R.; Riu, F.; Murineddu, G.; Sanna, G.; Madeddu, S.; Delogu, I.; Loddo, R.; Carta, A.. - In: MEDICINAL CHEMISTRY. - ISSN 1573-4064. - 16:5(2020), pp. 677-688. [10.2174/1573406416666191226142744]

Preliminary anti-coxsackie activity of novel 1-[4-(5,6-dimethyl(h)1h(2h)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas

Piras S.;Corona P.;Ibba R.;Riu F.;Murineddu G.;Sanna G.;Madeddu S.;Loddo R.;Carta A.
2020

Abstract

Background: Coxsackievirus infections are associated with cases of aseptic meningitis, encephalitis, myocarditis, and some chronic disease. Method: 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)]. Result: 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.
Preliminary anti-coxsackie activity of novel 1-[4-(5,6-dimethyl(h)1h(2h)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas / Piras, S.; Corona, P.; Ibba, R.; Riu, F.; Murineddu, G.; Sanna, G.; Madeddu, S.; Delogu, I.; Loddo, R.; Carta, A.. - In: MEDICINAL CHEMISTRY. - ISSN 1573-4064. - 16:5(2020), pp. 677-688. [10.2174/1573406416666191226142744]
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11388/236033
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