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李刚,博士,副研究员,硕士生导师。2012年7月毕业于北京协和医学院,获药物化学专业博士学位。2012年8月在中国医学科学院药物研究所合成药物化学室工作至今,先后任助理研究员、副研究员。主要从事药物化学、新药研发及有机合成方法学等方面的研究。主要研究方向包括代谢性疾病及耐药结核病的创新药物研究,金属催化的芳杂环合成方法学研究。目前已发表研究论文24篇,其中第一作者7篇,通讯作者10篇,SCI收录21篇。申请发明专利12项,其中获授权专利4项。2017年获得药物所2016年度“梁周黄于刘”青年科技二等奖。2020年获得药物所第六届青年教师教学基本功比赛二等奖,北京协和医学院第十一届青年教师教学基本功比赛三等奖。目前是Journal of Medicinal Chemistry、European Journal of Medicinal Chemistry和Advanced Synthesis & Catalysis等杂志的审稿人。
教育背景:
2009/9–2012/7,北京协和医学院,药物化学,博士
2006/9–2009/7,南昌大学医学院,药物化学,硕士
2002/9–2006/7,安徽工业大学,应用化学,学士
工作经历:
2016/10-至今,中国医学科学院药物研究所,合成药物化学室,副研究员
2012/8-2016/9,中国医学科学院药物研究所,合成药物化学室,助理研究员
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支持扩展名:.rar .zip .doc .docx .pdf .jpg .png .jpeg近年来,主持承担“重大新药创制”国家科技重大专项子课题、国家自然科学基金青年基金、中国药学会-以岭生物医药创新基金和中央公益性科研院所基本科研业务费等项目,并作为主要研究人员参与了国家“十二五”和“十三五”重大新药创制专项课题、中国医学科学院创新工程重大协同创新项目及与企业合作的开发项目等多项课题。
代表性论文:
1、Pengxu Wang∥, Sarah M. Batt∥, Bin Wang, Lei Fu, Rongfei Qin, Yu Lu, Gang Li*, Gurdyal S. Besra*, Haihong Huang*.Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities. J. Med. Chem., 2021, 64, 6241–6261. (Supplementary Cover)
2、Peng Li, Bin Wang, Lei Fu, Kaijing Guo, Chen Ma,Baolian Wang, Ziyun Lin, Gang Li*, Haihong Huang*, Yu Lu*. Identification of novelbenzothiopyranones with ester and amide motifs derived from active metaboliteas promising leads against Mycobacterium tuberculosis. Eur. J. Med. Chem., 2021, 222, 113603.
3、Hui Chen, Bin Wang, Peng Li, Hong Yan, Gang Li*, Haihong Huang*, Yu Lu*. The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP2C9 inhibition. Bioorg. Med. Chem. Lett., 2021, 40, 127924.
4、Peng Li, Shengnan Li, Gang Li*, Haihong Huang*. Synthesis of 2-Aryl-4H-thiochromen-4-one Derivatives via a Cross-Coupling Reaction. ACS Omega, 2021, 6, 14655−14663.
5、Gang Li#, Bingxu Meng#, Baokun Yuan, Yi Huan,Tian Zhou, Qian Jiang, Lei Lei, Li Sheng, Weiping Wang, Ningbo Gong, Yang Lu, Chen Ma, Yan Li, Zhufang Shen*, Haihong Huang*. The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119. Eur. J. Med. Chem., 2020, 188, 112017.
6、Hui Chen, Peng Li, Rongfei Qin, Hong Yan, Gang Li*, Haihong Huang*. DMAP catalyzed one-pot synthesis of quinazoline-2,4-diones from 2-aminobenzamides and di-tert-butyl dicarbonate. ACS Omega, 2020, 5, 9614−9623.
7、Peng Li, Yongqi Wu, Tingting Zhang, Chen Ma, Ziyun Lin, Gang Li* and Haihong Huang*. An efficient and concise access to 2-amino-4H-benzothiopyran-4-one derivatives. Beilstein J. Org. Chem., 2019, 15, 703–709.
8、 Peng Li, Bin Wang, Xinwei Zhang, Sarah M.Batt, Gurdyal S. Besra, Tingting Zhang, Chen Ma, Dongfeng Zhang, Ziyun Lin, Gang Li*, Haihong Huang*, Yu Lu*. Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones. Eur. J. Med. Chem., 2018, 160, 157-170.
9、Peng-Xu Wang, Ya-Nan Wang, Zi-Yun Lin, Gang Li*, and Hai-Hong Huang*. Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation. Synth. Commun., 2018, 48(10), 1183-1189.
10、Gang Li#, Yi Huan#, Baokun Yuan, Jin Wang, Qian Jiang, Ziyun Lin, Zhufang Shen*, Haihong Huang*. Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents. Eur.J. Med. Chem., 2016, 124, 103-116.
11、Gang Li#, Bao-Kun Yuan#, Wu Tang, Hong-Yi Zhao, Zi-Yun Lin, Hai-HongHuang*, An improved and efficient synthesis of the antibacterial agent torezolid, Chem. Pharm. Bull., 2015, 63, 143-146.
12、Gang Li, Li Li, Haihong Huang* and Dali Yin*. Ti(IV)-catalyzed cascade synthesis of tetrahydrofuro[3,2-d]oxazole from arene-1,4-diones. Org. Biomol. Chem., 2015, 13, 4418-4421.
13、Gang Li, Jin Wang, Baokun Yuan, Dongfeng Zhang, Ziyun Lin, Peng Li, Haihong Huang*. Iron-catalyzed one-pot synthesis of benzimidazoles from 2-nitroanilines and benzylic alcohols. Tetrahedron Lett., 2013, 54, 6934-6936.
专利:
获得4项国内专利授权。
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