Flexible Synthesis and Evaluation of Diverse Anti-Apicomplexa Cyclic Peptides

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• 作者：Mariam Traor茅 ; Flore Mietton ; Dani猫le Maubon ; Marine Peuchmaur ; Flaviane Francisco Hil谩rio ; Rossimiriam Pereira de Freitas ; Alexandre Bougdour ; Aur茅lie Curt ; Marjorie Maynadier ; Henri Vial ; Herv茅 Pelloux ; Mohamed-Ali Hakimi ; Yung-Sing Wong
• 刊名：The Journal of Organic Chemistry
• 出版年：2013
• 出版时间：April 19, 2013
• 年：2013
• 卷：78
• 期：8
• 页码：3655-3675
• 全文大小：831K
• 年卷期：v.78,no.8(April 19, 2013)
• ISSN：1520-6904

文摘

A modular approach to synthesize anti-Apicomplexa parasite inhibitors was developed that takes advantage of a pluripotent cyclic tetrapeptide scaffold capable of adjusting appendage and skeletal diversities in only a few steps (one to three steps). The diversification processes make use of selective radical coupling reactions and involve a new example of a reductive carbon鈥搉itrogen cleavage reaction with SmI₂. The resulting bioactive cyclic peptides have revealed new insights into structural factors that govern selectivity between Apicomplexa parasites such as Toxoplasma and Plasmodium and human cells.