Synthesis of new spirooxindole derivatives through 1,3-dipolar cycloaddition of azomethine ylides and their antitubercular activity

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• 作者：Fadwa Rouatbi^a ; Moheddine Askri^a ; ^{moheddine.askri@fsm.rnu.tn" class="auth_mail" title="E-mail the corresponding author} ; Frederic Nana^b ; Gilbert Kirsch^b ; Dharmarajan Sriram^c ; Perumal Yogeeswari^c
• 关键词：(E ; E)-1 ; 3-Bis(arylidene)indan-2-one ; 1 ; 3-Dipolar cycloaddition ; Azomethine ylide ; Mycobacterium tuberculosis
• 刊名：Tetrahedron Letters
• 出版年：2016
• 出版时间：13 January 2016
• 年：2016
• 卷：57
• 期：2
• 页码：163-167
• 全文大小：914 K

文摘

Non-stabilized azomethine ylides, generated in situ from isatin derivatives and l-proline, have been reacted with (E,E)-1,3-bis(arylidene)indan-2-ones as dipolarophiles in a 1,3-dipolar cycloaddition reaction. Novel functionalized dispiroheterocyclic compounds were obtained with low diastereoselectivity and the regiochemical outcome of the cycloaddition reaction was confirmed by single crystal X-ray analysis. The compounds were investigated by in vitro screening against Mycobacterium tuberculosis (MIC) using the agar dilution method and displayed good activities.