Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains

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• 作者：Ziqiang Li^a ; ^&dagger ; ; Xiaoguang Bai^b ; ^&dagger ; ; Qi Deng^b ; Guoning Zhang^b ; Lei Zhou^b ; Yishuang Liu^b ; Juxian Wang^b ; ^{imbjxwang@163.com} ; Yucheng Wang^b ; ^{wyc9999@gmail.com}
• 关键词：Shikimate dehydrogenase ; Antitubercular agent ; 3 ; 6-Disubstituted triazolothiadiazine ; SAR
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：25
• 期：1
• 页码：213-220
• 全文大小：709 K
• 卷排序：25

文摘

Antitubercular 3,6-disubstituted triazolothiadiazines were designed and synthesized. Preliminary SAR of 3,6-disubstituted triazolothiadiazines was described. Compounds 6c-3 and 6g-3 show exceptional antitubercular potency and no cytotoxicity. Compounds 6c-3 and 6g-3 may be promising multidrug-resistance-reversing agents.