Tyrosol and hydroxytyrosol derivatives as antitrypanosomal and antileishmanial agents
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- 作者：Efres Belmonte-Rechea ; Marta Martí ; nez-Garcí ; aa ; Pablo Peñ ; alvera ; b ; Veró ; nica Gó ; mez-Pé ; reza ; Ricardo Lucasa ; b ; Francisco Gamarroa ; José ; Marí ; a Pé ; rez-Victoriaa ; josepv@ipb.csic.es" class="auth_mail" title="E-mail the corresponding author ; Juan Carlos Moralesa ; b ; jcmorales@ipb.csic.es" class="auth_mail" title="E-mail the corresponding author
- 关键词：Antitrypanosomal ; Antileishmanial ; Tyrosol ; Hydroxytyrosol
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：25 August 2016
- 年：2016
- 卷：119
- 期：Complete
- 页码：132-140
- 全文大小：578 K
文摘
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Tyrosol and hydroxytyrosol alkyl derivatives were synthesized in 2–3 steps.
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Their antitrypanosomal and antileishmanial activity is reported.
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Compounds 13 and 14 showed the best IC50 against Trypanosoma brucei (0.36–0.6 μM).
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Compounds 13 and 14 displayed a high selectivity index (SI = 101–118).
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Two phenol groups and medium size alkyl chain are essential for activity.