Reaction of rosmarinic acid with nitrite ions in acidic conditions: Discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents
Reaction of rosmarinic acid with nitrite ions in acidic conditions: Discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents
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DOI:
10.1021/jm7011134
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发表时间:
2008-04-24
影响因子:
7.3
通讯作者:
Cotelle, Philippe
中科院分区:
文献类型:
--
作者:
Dubois, Manie;Bailly, Fabrice;Cotelle, Philippe
Rosmarinic acid was reacted with nitrite ions under acidic conditions to give 6'-nitro- and 6',6 ''-dinitrorosmarinic acids according to the reaction time. Both compounds were active as HIV-1 integrase inhibitors at the submicromolar level. They also inhibited the viral replication in MT-4 cells with modest and similar selectivity indexes. The nitration of rosmarinic acid strongly improves the anti-integrase inhibition and the antiviral activity without increasing the cellular toxicity.