期刊
CHEMISTRY & BIODIVERSITY
卷 15, 期 7, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201800134
关键词
benzofuran neolignans; neglected diseases; oxidative coupling; phenylpropanoids; Schistosoma mansoni
资金
- Brazilian foundations FundacAo de Amparo a Pesquisa do Estado de SAo Paulo [13/20094-0, 13/11164-4, 09/12202-1, 14/50265-3, 16/24456-1]
- Conselho Nacional de Desenvolvimento Cientufico e Tecnologico
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [14/50265-3, 13/11164-4, 09/12202-1] Funding Source: FAPESP
We have evaluated the antischistosomal activity of synthetic dihydrobenzofuran neolignans (DBNs) derived from (+/-)-trans-dehydrodicoumaric acid dimethyl ester (1) and (+/-)-trans-dehydrodiferulic acid dimethyl ester (2) against adult Schistosoma mansoni worms invitro. Compound 4 ((+/-)-trans-4-O-acetyldehydrodiferulic acid dimethyl ester) displayed the most promising activity; at 200m, it kills 100 +/- 0% of worms after 24h, which resembles the result achieved with praziquantel (positive control) at 1.56m. The hydrogenation of the double bond between C7 and C8, the introduction of an additional methyl group at C3, and a double bond between C7 and C8 decreased the schistosomicidal activity of DBNs. On the other hand, the presence of the acetoxy group at C4 played an interesting role in this activity. These results demonstrated the interesting schistosomicidal potential of DBNs, which could be further exploited.
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