黄海洪 研究员,博士生导师。中国医学科学院抗耐药结核创新药物研究重点实验室主任,第九届中国药学会抗生素专业委员会委员。长期以来主要从事耐药结核、自身免疫、代谢性疾病、恶性肿瘤等重大疾病领域的创新药物研究。自2002年起先后主持承担两项科技部“863”计划课题、四项国家新药创制科技重大专项课题、国家自然科学基金和北京市自然科学基金课题各一项、两项北京市科委创新药物临床前研究课题、两项抗结核新药研发国际合作项目,以及多项企业委托新药研发项目等。其中抗类风湿性关节炎1类新药盐酸氯苯哌酮、抗耐药结核1类新药吡法齐明已进入临床研究、抗耐药结核1类新药OTB-658于2020年12月获得NMPA签发的药物临床试验批准。
1. 药物分子设计与合成
2. 活性天然产物的结构优化
3. 针对重大疾病(耐药结核、自身免疫、代谢性疾病及恶性肿瘤等)的创新药物研究
1. Dongfeng Zhang ∇, Peng Li ∇, Yongxin Gao, Yaoyao Song, Yaqin Zhu, Hong Su, Beibei Yang, Li Li, Gang Li, Ningbo Gong, Yang Lu, Huanjie Shao*, Chunrong Yu*, Haihong Huang*, Discovery of a Candidate Containing an (S) 3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro
1H inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia. J. Med. Chem., 2021, 64, 7434−7452.
2. 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.
3. Yongqi Wu, Bin Wang, Haijia Lu, Hongyi Zhao, Beibei Yang, Yu Lu, Dongfeng Zhang*, Ning Sun*, Haihong Huang*. Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens. J. Med. Chem., 2021, 64, 3234−3248.
4. 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.
5. Hongyi Zhao, Bin Wang, Lei Fu, Gang Li, Haijia Lu, Yuke Liu, Li Sheng, Yan Li, Baoxi Zhang, Yang Lu, Chen Ma, Haihong Huang,* Dongfeng Zhang,* and Yu Lu*. Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis. J. Med. Chem., 2020, 63, 9316−9339.
6. 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., 188(2020) 112017.
7. Hongyi Zhao, Wenting Zhao, Shihao Cheng, Haijia Lu, Dongfeng Zhang* and Haihong Huang*, Efficient and stereoselective one-pot synthesis of benzo[b]oxazolo[3,4-d][1,4]oxazin-1-ones. RSC Adv., 2020, 10, 24037.
8. Dongfeng Zhang, Yun Lin, Xi Chen, Wenting Zhao, Dongni Chen, Meng Gao, Qinglin Wang, Bin Wang, Haihong Huang*, Yongjun Lu*, and Yu Lu*. Docking- and Pharmacophore-Based Virtual Screening for the Identification of Novel Mycobacterium tuberculosis Protein Tyrosine Phosphatase B (MptpB) Inhibitor with A Thiobarbiturate Scaffold. Bioorganic Chemistry, 2019, 85, 229-239.
9. Meng Gao, Wenting Zhao, Hongyi Zhao, Ziyun Lin, Dongfeng Zhang* and Haihong Huang*. An efficient and facile access to highly functionalized pyrrole derivatives. Beilstein J. Org. Chem., 2018, 14, 884-890.
10. 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. Synthetic Communications, 2018, 48(10), 1183-1189.
11. 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.
12. Hongyi Zhao, Yu Lu, Li Sheng, Zishuo Yuan, Bin Wang, Weiping Wang, Yan Li, Chen Ma, Xiaoliang Wang, Dongfeng Zhang*, and Haihong Huang*. Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis. ACS Med. Chem. Lett., 2017, 8, 533-537.
13. 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.
14. Peng Li, Xinwei Zhang, Yongqi Wu, Maosheng Cheng, Dongfeng Zhang, Gang Li, Ziyun Lin, Xiang Zhang*, Haihong Huang*. A facile and efficient synthesis of 4H-1,3-benzoxazine-4-one with electron-withdrawing group derivatives. Tetrahedron Letters, 2015, 56, 4683-4685.
15. 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.
16. Chenshu Lu, Ke Tang, Yan Li, Peng Li, Ziyun Lin, Dali Yin, Xiaoguang Chen* and Haihong Huang*. Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents. Eur. J. Med. Chem., 2014, 77, 351-360.
17. LUO Can, TANG Ke, LI Yan, YIN DaLi, CHEN XiaoGuang* & HUANG HaiHong*. Design, Synthesis and in vitro Antitumor Evaluation of Novel Diaryl Urea Derivatives Bearing Sulfonamide Moiety. SCIENCE CHINA CHEMISTRY, 2013, 56(11), 1564-1572.
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 Letters, 2013, 54(50), 6934-6936.
19. Chun Lin Zhang, Dong Feng Zhang, Hong Yi Zhao, Zi Yun Lin, Hai Hong Huang*. A facile protocol for N-Cbz protection of amines in PEG-600. Chinese Chemical Letters, 2012, 23, 789-792.
20. Dongfeng Zhang#, Yu Lu#, Kai Liu, Binna Liu, Jingbin Wang, Gang Zhang, Hao Zhang, Yang Liu, Bin Wang, Meiqin Zheng, Lei Fu, Yanyan Hou, Ningbo Gong, Yang Lv, Chun Li, Christopher B. Cooper, Anna M. Upton, Dali Yin, Zhenkun Ma*, and Haihong Huang*. Identification of Less Lipophilic Riminophenazine Derivatives for the Treatment of Drug-Resistant Tuberculosis.
J. Med. Chem., 2012, 55(19), 8409-8417.