科研队伍

李刚,博士,副研究员,硕士生导师,中国研究型医院学会结核病学专业委员会委员,《中国药物化学杂志》首届青年编委。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。主要研究方向包括耐药结核病及代谢性疾病的创新药物研究。近年来,主持承担“重大新药创制”国家科技重大专项子课题、国家自然科学基金面上/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。目前已发表研究论文30余篇,代表性工作发表在J. Med. Chem.和Eur. J. Med. Chem.等著名药物化学期刊。申请发明专利18项,其中获授权专利11项。2023年获得中国医学科学院北京协和医学院首届创新转化潜力大赛,生物医药组三等奖。2020年获得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。2017年获得药物研究所“梁周黄于刘”青年科技二等奖。

1. 药物分子设计合成及成药性研究
2. 创新药物研发及合成工艺研究
3. 有机合成方法学研究

1. Shengnan Li#, Hui Liao#, Lijun Luo#, Bingxu Meng, Fengxin Zheng, Li Sheng, Hongyi Zhao, Yi Huan, Lei Lei, Jiayu Zhai, Kunlu Zhao, Jinhong Tian, Ting Wu, Gang Li,* Jianxin Pang,* Haihong Huang*. Proline-derived quinoline formamide compounds as human urate transporter 1 inhibitors with potent uric acid-lowering activities. Eur. J. Med. Chem., 2024, 269, 116327.
2. 唐霞霞,李文艺,李鹏,王彬,陆宇,黄海洪*,李刚*. 2-芳基取代苯并硫代吡喃酮类化合物的设计、合成及其抗结核活性研究[J]. 药学学报, 2024, 59 (4): 987−996.
3. Peng Li#, Kaijing Guo#, Lei Fu, Bin Wang, Baoxi Zhang, Ningbo Gong, Yang Lu, Chen Ma, Haihong Huang*, Yu Lu*, Gang Li*. Solubility-driven optimization of benzothiopyranone salts leading to a preclinical candidate with improved pharmacokinetic properties and activity against Mycobacterium tuberculosis. Eur. J. Med. Chem., 2023, 246, 114993.
4. Peng Li, Bin Wang, Xi Chen, Ziyun Lin, Gang Li*, Yu Lu*, Haihong Huang*. Design, synthesis and biological evaluation of alkynyl-containing maleimide derivatives for the treatment of drug-resistant tuberculosis. Bioorg. Chem., 2023, 131, 106250.
5. Rongfei Qin#, Pengxu Wang#, Bin Wang, Lei Fu, Sarah M. Batt, Gurdyal S. Besra, Chengwei Wu, Yanan Wang, Haihong Huang*, Yu Lu*, Gang Li*, Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis, Eur. J. Med. Chem., 2022, 231, 114145.
6. 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)
7. Peng Li, Bin Wang, Lei Fu, Kaijing Guo, Chen Ma, Baolian Wang, Ziyun Lin, Gang Li*, Haihong Huang*, Yu Lu*. Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis. Eur. J. Med. Chem., 2021, 222, 113603.
8. 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 CYP 2C9 inhibition. Bioorg. Med. Chem. Lett., 2021, 40, 127924.
9. 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.
10. 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.
11. 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.
12. Peng Li, Yongqi Wu, Tingting Zhang, Chen Ma, Ziyun Lin, Gang Li*, Haihong Huang*. An efficient and concise access to 2-amino-4H-benzothiopyran-4-one derivatives. Beilstein J. Org. Chem., 2019, 15, 703–709.
13. 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.
14. Pengxu Wang, Yanan Wang, Ziyun Lin, Gang Li*, HaiHong Huang*. Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation. Synth. Commun., 2018, 48(10), 1183-1189.
15. 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.
16. Gang Li1, Bao-Kun Yuan1, Wu Tang, Hong-Yi Zhao, Zi-Yun Lin, Hai-Hong Huang*, An improved and efficient synthesis of the antibacterial agent torezolid, Chem. Pharm. Bull., 2015, 63, 143-146.
17. 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.
18. 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.

申请发明专利18项,其中PCT专利1项,已进入国家阶段,获授权专利11项。