Browsing by Author "Wang, Apeng"

Now showing 1 - 3 of 3
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    Design, synthesis and antimycobacterial activity of novel nitrobenzamide derivatives
    (Elsevier, 2018) Wang, Hongjian; Lv, Kai; Li, Xiaoning; Wang, Bo; Wang, Apeng; Tao, Zeyu; Geng, Yunhe; Wang, Bin; Huang, Menghao; Liu, Mingliang; Guo, Huiyuan; Lu, Yu; Medicine, School of Medicine
    We report herein the design and synthesis of a series of novel nitrobenzamide derivatives. Results reveal that many of them display considerable in vitro antitubercular activity. Four N-benzyl or N-(pyridine-2-yl)methyl 3,5-dinitrobenzamides A6, A11, C1 and C4 have not only the same excellent MIC values of <0.016 μg/mL against both drug-sensitive MTB strain H37Rv and two drug-resistant clinical isolates as PBTZ169 and the lead 1, but also acceptable safety indices (SI > 1500), opening a new direction for further development.
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    Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety
    (Elsevier, 2018-05) Lv, Kai; Tao, Zeyu; Liu, Qian; Yang, Lu; Wang, Bin; Wu, Shuo; Wang, Apeng; Huang, Menghao; Liu, Mingliang; Lu, Yu; Medicine, School of Medicine
    We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 μg/mL) against drug-susceptible Mycobacterium tuberculosis H37RV strain. After two set of modifications, compound 2i were found to display comparable in vitro anti-TB activity (MIC < 0.016 μg/mL) to PBTZ169 against drug-sensitive and resistant mycobacterium tuberculosis strains. Compound 2i also showed acceptable PK profiles. Studies to determine PK profiles in lung and in vivo efficacy of 2i are currently under way.
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    Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives
    (Elsevier, 2018-09) Tao, Zeyu; Cao, Ruiyuan; Yan, Yunzheng; Huang, Guocheng; Lv, Kai; Li, Wei; Geng, Yunhe; Zhao, Lei; Wang, Apeng; He, Qinhao; Yang, Jingjing; Fan, Shiyong; Huang, Menghao; Guo, Huiyuan; Zhong, Wu; Lu, Mingliang; Medicine, School of Medicine
    We report herein the design and synthesis of a series of novel Sinefungin (SIN) derivatives, based on the structures of SIN and its analogue EPZ004777. Our results reveal that target compounds 1ad-af, 1ba-bb and 1bf-bh show better activity (IC50 = 4.56–20.16 μM) than EPZ004777 (IC50 = 35.19 μM). Surprisingly, SIN was founded to be not as active (IC50 > 50 μM) as we and other research groups predicted. Interestingly, the intermediates 9a-b and 11b display potent anti-ZIKV potency (IC50 = 6.33–29.98 μM), and compound 9a also exhibits acceptable cytotoxicity (CC50 > 200 μM), suggesting their promising potential to be leads for further development.