Structure-activity relationship studies on a Trp dendrimer with dual activities against HIV and enterovirus A71. Modifications on the amino acid

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• 作者：Bel&eacute ; n Martí ; nez-Gualdap>ap> ; Liang Sunp>bp> ; Eva Rivero-Bucetap>ap>p> ; p>p>1p> ; Aida Floresp>ap>p> ; p>p>2p> ; Ernesto Quesadap>ap> ; Jan Balzarinip>bp> ; Sam Noppenp>bp> ; Sandra Liekensp>bp> ; Dominique Scholsp>bp> ; Johan Neytsp>bp> ; Pieter Leyssenp>bp> ; Carmen Mirabellip>bp> ; Marí ; a-Jos&eacute ; Camarasap>ap> ; Ana San-F&eacute ; lixp>ap>p> ; p>p>anarosa@iqm.csic.esp>
• 关键词：Antiviral agents ; AIDS ; HFMD ; HIV ; EV71 ; Tryptophan
• 刊名：Antiviral Research
• 出版年：2017
• 出版时间：March 2017
• 年：2017
• 卷：139
• 期：Complete
• 页码：32-40
• 全文大小：1223 K
• 卷排序：139

文摘

Novel dendrimers containing different amino acids on the periphery have been synthesized. These compounds have dual action against HIV and EV71. Tyrosine dendrimer is the most potent against EV71 while dendrimer with N-methyl Trp is the most potent against HIV-1. Dendrimer with tyrosine is an extremely highly potent inhibitor of clinical EV71 isolates (nanoMolar-picoMolar potency). Presence of hydrophilic groups (NH, OH) on the aromatic ring of the amino acid is beneficial for anti-EV71 activity.