微生物与生化药学方向

吕凯

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时间:2021-07-07    

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吕凯   有机化学室   副研究员   硕士生导师

2017/08-至今 世界杯在哪里买球 副研究员

2016/04-2017/07 世界杯在哪里买球 助理研究员

2015/11-2016/04 河北医科大学药学院 讲师

2012/10-2015/10 普渡大学化学院 博士后


2009/09-2012/07 北京协和医学院 微生物与生化药学 博士

2006/09-2009/07 河北医科大学-军事医学科学院 药物化学 联合培养硕士

2002/09-2006/07 河北医科大学 药学 学士

主要研究方向:抗病毒、抗结核、以及抗耐药菌小分子的药物化学研究

专业研究领域:主要开展抗感染药物化学相关研究,侧重于抗病毒、抗菌、以及抗结核药物候选物的发现。我们基于构效关系,以及结构的/配体的计算机辅助药物方法对先导化合物开展结构优化。所有目标化合物经化学方法合成并开展体外活性评价。优选化合物开展药代动力学,毒理学,以及体内药效学评价从而初步确定候选化合物。本课题组的化合物TZY-5-84,体内外具有优秀的抗结核活性,且表现出了较好的成药性。此外,本课题组还开展药物合成新方法,新工艺的研究。

代表性论文:

1K. Lv, S. Wu, W. Li, Y. Geng, M. Wu, J. Zhou, Y. Li, Q. Gao, M. Liu, Design, synthesis and anti-HBV activity of NVR3-778 derivatives, Bioorganic chemistry, 94 (2020) 103363.

2K. Lv, W. Li, S. Wu, Y. Geng, A. Wang, L. Yang, M. Huang, K. Chowdhury, Y. Li, M. Liu, Amino acid prodrugs of NVR3-778: Design, synthesis and anti-HBV activity, Bioorganic & medicinal chemistry letters, 30 (2020) 127103.

3H. Wang, K. Lv (Co-first author),, X. Li, B. Wang, A. Wang, Z. Tao, Y. Geng, B. Wang, M. Huang, M. Liu, H. Guo, Y. Lu, Design, synthesis and antimycobacterial activity of novel nitrobenzamide derivatives, Chinese Chemical Letters, 30 (2019) 413-416.

4A. Wang, K. Lv (Co-first author),, Z. Tao, J. Gu, L. Fu, M. Liu, B. Wan, S.G. Franzblau, C. Ma, X. Ma, B. Han, A. Wang, S. Xu, Y. Lu, Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents, European journal of medicinal chemistry, 181 (2019) 111595.

5A. Wang, K. Lv (Co-first author),, L. Li, H. Liu, Z. Tao, B. Wang, M. Liu, C. Ma, X. Ma, B. Han, A. Wang, Y. Lu, Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents, European journal of medicinal chemistry, 178 (2019) 715-725.

6K. Lv, A. Wang, Z. Tao, L. Fu, H. Liu, B. Wang, C. Ma, H. Wang, X. Ma, B. Han, A. Wang, K. Zhang, M. Liu, Y. Lu, hERG optimizations of IMB1603, discovery of alternative benzothiazinones as new antitubercular agents, European journal of medicinal chemistry, 179 (2019) 208-217.

7Z. Tao, R. Cao, Y. Yan, G. Huang, K. Lv*, W. Li, Y. Geng, L. Zhao, A. Wang, Q. He, J. Yang, S. Fan, M. Huang, H. Guo, W. Zhong, M. Liu, Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives, European journal of medicinal chemistry, 157 (2018) 994-1004.

8K. Lv, Z. Tao, Q. Liu, L. Yang, B. Wang, S. Wu, A. Wang, M. Huang, M. Liu, Y. Lu, Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety, European journal of medicinal chemistry, 151 (2018) 1-8.

9L. Li, K. Lv (Co-first author), Y. Yang, J. Sun, Z. Tao, A. Wang, B. Wang, H. Wang, Y. Geng, M. Liu, H. Guo, Y. Lu, Identification of N-Benzyl 3,5-Dinitrobenzamides Derived from PBTZ169 as Antitubercular Agents, ACS medicinal chemistry letters, 9 (2018) 741-745.

10R. Zhang, K. Lv (Co-first author), B. Wang, L. Li, B. Wang, M. Liu, H. Guo, A. Wang, Y. Lu, Design, synthesis and antitubercular evaluation of benzothiazinones containing an oximido or amino nitrogen heterocycle moiety, Rsc Adv, 7 (2017) 1480-1483.

11L. Tang, Z. Bei, Y. Song, L. Xu, H. Wang, D. Zhang, Y. Dou, K. Lv*, H. Wang, Synthesis and in vivo antimalarial activity of novel naphthoquine derivatives with linear/cyclic structured pendants, Future medicinal chemistry, 9 (2017) 1117-1127.

12K. Lv, X. You, B. Wang, Z. Wei, Y. Chai, B. Wang, A. Wang, G. Huang, M. Liu, Y. Lu, Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents, ACS medicinal chemistry letters, 8 (2017) 636-641.

13K. Lv, L. Li, B. Wang, M. Liu, B. Wang, W. Shen, H. Guo, Y. Lu, Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives, European journal of medicinal chemistry, 137 (2017) 117-125.

专利:

1、刘明亮,吕凯,钟武,曹瑞源,闫赟政,陶泽宇,和青昊,王洪建,李薇,耿云鹤,一种核苷类化合物及其制备方法和治疗黄病毒感染的药物组合物CN201810941785.0, 授权日:2020.03.10

2、刘明亮,吕凯,曹瑞源,汪阿鹏,闫赟政,陶泽宇,李微,耿云鹤,杨晶晶,赵磊,李月香, 一种西奈芬净类似物及其制备方法,CN201810074544.0,授权日:2020.09.10

3、刘明亮,蒋建东,李玉环,吕凯,马西灿,二氢喹嗪酮酸类化合物及其应用,CN201911063354.X,申请人:2019.11.04

4、刘明亮,李玉环,陶泽宇,蒋建东,吕凯,吴硕,汪阿鹏,杨璐,含有环丙基片段的吡唑并吡嗪甲酰胺类化合物及其应用,CN2019111039949, 申请日:2019.11.13

5、陆宇,刘明亮,汪阿鹏,吕凯,郭慧元,王洪建,陶泽宇, 含有碱性稠环片段的咪唑并[1,2-a]吡啶-3-酰胺类化合物及其制备方法, CN2018103700545, 申请日:2018.04.24, 授权公告日:2020.06.19

6、刘明亮,汪阿鹏,吕凯,郭慧元,陶泽宇,王洪建,陈仕洪, 含有肟基片段的苯并噻嗪-4-酮类化合物及其制备方法, CN2018102848615, 申请日:2018.04.02, 授权公告日:2020.05.15

7、陆宇,刘明亮,吕凯,黄国成,汪阿鹏,王洪建,陶泽宇,郭慧元,含有异吲哚啉片段的35-二硝基苯甲酰胺类化合物及其制备方法,CN201710894507.x 申请日:2017-09-28,授权公告日:2020.01.17

8、刘明亮,郭慧元,吕凯,汪阿鹏,黄国成,陶泽宇,王洪建,刘洪涛,魏增泉,陈仕洪, 含有碱性桥环片段的苯并噻嗪-4-酮类化合物及其制备方法,CN2017104120720 , 申请日:2017.06.02, 授权公告日:2020.05.19

9、刘明亮,郭慧元,吕凯,汪阿鹏,黄国成,陶泽宇,王洪建,李霄宁,张俊,陈仕洪,含有2,7-二氮杂螺[3.5]壬烷片段的苯并噻嗪-4-酮类化合物及其制备方法, CN 201710121170.9 (申请日:2017-03-02)授权公告日:2019.09.17

10、刘明亮,郭慧元,吕凯,汪阿鹏,柴芸,黄国成,陶泽宇,李霄宁,陈仕洪,含有2,8-二氮杂螺[4.5]癸烷片段的苯并噻嗪-4-酮类化合物及其制备方法, CN 201710121169.9(申请日:2017-03-02)授权公告日:2019.09.13

联系电话:010-63165280

电子邮箱:lvkai@imb.pumc.edu.cn

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世界杯买球-世界杯在哪里买球「2022年卡塔尔世界杯」

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世界杯买球-世界杯在哪里买球「2022年卡塔尔世界杯」