Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds

详细信息    查看全文

• 作者：Chiara Borsarip>ap> ; Nuno Santaremp>bp> ; Juan Torradop>cp> ; Ana Isabel Olí ; asp>cp>p> ; p>p>ep> ; Marí ; a Jesú ; s Corralp>cp>p> ; p>p>ep> ; Catarina Baptistap>bp> ; Sheraz Gulp>dp> ; Markus Wolfp>dp> ; Maria Kuzikovp>dp> ; Bernhard Ellingerp>dp> ; Gesa Wittp>dp>p> ; p>p>Gesa.Witt@ime.fraunhofer.dep> ; Philip Gribbonp>dp>p> ; p>p>Philip.Gribbon@ime.fraunhofer.dep> ; Jeanette Reinshagenp>dp> ; Pasquale Lincianop>ap> ; Annalisa Taitp>ap> ; Luca Costantinop>ap> ; Lucio H. Freitas-Juniorp>fp> ; Carolina B. Moraesp>fp> ; Pascoalino Bruno dos Santosp>fp> ; Laura Maria Alcâ ; ntarap>fp> ; Caio Haddad Francop>fp> ; Claudia Danielli Bertolacinip>fp> ; Vanessa Fontanap>fp> ; Paloma Tejera Nevadop>gp> ; Joachim Closp>gp> ; José ; Marí ; a Alundap>cp>p> ; p>p>ep> ; Anabela Cordeiro-da-Silvap>bp> ; Stefania Ferrarip>ap> ; Maria Paola Costip>ap>p> ; p>p>mariapaola.costi@unimore.itp>
• 关键词：Chalcones ; Trypanosoma brucei ; Trypanosoma cruzi ; Leishmania infantum ; Early toxicity studies ; Cyclodextrins formulation
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：1129-1135
• 全文大小：709 K
• 卷排序：126

文摘

Thirteen 2’-hydroxy methoxylated chalcones were synthesized. Compounds 1, 3, 4, 7 and 8 showed higher potency than flavokawin B towards T. brucei. A panel of in vitro early toxicological properties was evaluated. The formulation of compound 4 with cyclodextrins increased the oral bioavailability by 7.5 fold.