Studies on the trypanocidal activity of semi-synthetic pyran[b-4,3]naphtho[1,2-d]imidazoles from β-lapachone

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• 作者：Kelly C.G De Moura ; Kelly Salomã ; o ; Rubem F.S Menna-Barreto ; Flá ; vio S Emery ; Maria do Carmo F.R Pinto ; Antô ; nio V Pinto ; Solange L de Castro
• 关键词：Trypanosoma cruzi ; Chagas’ ; disease ; Naphthoquinones ; β ; -lapachone ; Naphthoimidazoles ; Chemotherapy
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2004
• 出版时间：July 2004
• 年：2004
• 卷：39
• 期：7
• 页码：639-645
• 全文大小：215 K

文摘

We synthesized new naphthoimidazoles from β-lapachone with an aromatic moiety linked to the imidazole ring, using phenylic and heterocyclic aldehydes. The most active compound against Trypanosoma cruzi had a p-methyl group linked to the phenyl ring, presenting an EC<sub>50sub> value of 15.5 ± 2.9 μM. No reliable correlation could be established with the biological activity and the structure of in the phenylic series. For the heterocyclic series, activity was associated with a three bond-distance from nitrogen to the imidazole ring, in accordance with our previous work.