Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds

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• 作者：Chiara Borsari^a ; Nuno Santarem^b ; Juan Torrado^c ; Ana Isabel Olí ; as^c ; ^e ; Marí ; a Jesú ; s Corral^c ; ^e ; Catarina Baptista^b ; Sheraz Gul^d ; Markus Wolf^d ; Maria Kuzikov^d ; Bernhard Ellinger^d ; Gesa Witt^d ; ^{Gesa.Witt@ime.fraunhofer.de} ; Philip Gribbon^d ; ^{Philip.Gribbon@ime.fraunhofer.de} ; Jeanette Reinshagen^d ; Pasquale Linciano^a ; Annalisa Tait^a ; Luca Costantino^a ; Lucio H. Freitas-Junior^f ; Carolina B. Moraes^f ; Pascoalino Bruno dos Santos^f ; Laura Maria Alcâ ; ntara^f ; Caio Haddad Franco^f ; Claudia Danielli Bertolacini^f ; Vanessa Fontana^f ; Paloma Tejera Nevado^g ; Joachim Clos^g ; José ; Marí ; a Alunda^c ; ^e ; Anabela Cordeiro-da-Silva^b ; Stefania Ferrari^a ; Maria Paola Costi^a ; ^{mariapaola.costi@unimore.it}
• 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.