期刊
ANTIVIRAL RESEARCH
卷 45, 期 3, 页码 199-210出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/S0166-3542(00)00072-3
关键词
isothiazole derivatives; antiviral; rhinovirus
A series of 3-methylthio-5-aryl-4-isothiazolecarbonitriles has been evaluated as anti rhinovirus agents against a panel. of 17 representative human rhinovirus (HRV) serotypes, belonging to both A and B groups. No anti rhinovirus activity was detected for 3-methylthio-5-phenyl-4-isothiazolecarbonitrile (IS-2). Isothiazole derivatives with bulky substituents (O-Bn or O-But groups) on the para position of the phenyl ring were the most effective compounds of this series. In fact, a reduction in virus-induced cytopathogenicity was demonstrated for the O-Bn substituted IS-50 compound against the majority (88%) of the rhinoviruses tested, whereas the compound with an O-Ts group (IS-44) was found to be a specific inhibitor of group B serotypes, exhibiting the lowest IC50 against HRVs type 2, 85 and 89. Our studies on the mechanism of action of IS-44 demonstrated that it prevents the thermal inactivation of HRV 2 infectivity, probably due to a conformational shift in the viral capsid and a decrease in affinity for the cellular receptor, resulting in an inhibition of attachment of the virions. (C) 2000 Elsevier Science B.V. All rights reserved.
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