Click-based synthesis and antitubercular evaluation of dibenzofuran tethered thiazolyl-1,2,3-triazolyl acetamides

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• 作者：Goverdhan Surineni^a ; Perumal Yogeeswari^b ; Dharmarajan Sriram^b ; Srinivas Kantevari^a ; ^c ; ^{kantevari@yahoo.com" class="auth_mail" title="E-mail the corresponding author} ; ^{kantevari@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Dibenzofuran ; Thiazole ; Triazole ; Antimycobacterial activity ; Tuberculosis
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 August 2016
• 年：2016
• 卷：26
• 期：15
• 页码：3684-3689
• 全文大小：1155 K

文摘

A series of novel dibenzofuran tethered thiazolyl-1,2,3-triazolyl acetamides, designed by assembling antitubercular pharmacophoric fragments, dibenzofuran, 2-aminothiazole and substituted triazoles in one molecular architecture, were evaluated against Mycobacterium tuberculosis. The new analogues class="boldFont">6a–class="boldFont">p accomplished in four step synthetic sequence utilizing click chemistry in the penultimate step, was fully characterized by their NMR and mass spectral data. Among the compounds class="boldFont">6a–class="boldFont">p screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv, three compounds class="boldFont">6j (MIC: 1.56 μg/mL); class="boldFont">6a and class="boldFont">6p (MIC: 3.13 μg/mL) was found to be most active and exhibited lower cytotoxicity. Among these three, class="boldFont">6j could be a candidate to consider as a drug like hit analogue for further development.