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黄海洪 中国医学科学院药物研究所合成药物化学研究室研究员,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。长期以来从事耐药结核、自身免疫、代谢性疾病、恶性肿瘤等治疗领域的创新药物研发工作,自2002年起先后主持承担两项国家科技部“863”计划课题、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、四项国家新药创制科技重大专项课题、两项抗结核新药研发国际合作项目、多项企业委托新药研发项目,以及医科院医学与健康科技创新工程等课题,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II期临床研究、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,抗肿瘤1类新药AST-1601已递交临床试验申请。
教育背景:
1985年9月-1989年7月 北京师范大学化学系 本科学士
1989年9月-1992年7月 南开大学化学系有机化学专业理学硕士
工作经历:
1992年8月 - 2004年8月 中国医学科学院药物研究所 实研、助研、副研
2004年9月 - 至今 中国医学科学院药物研究所 研究员
2009年2月 - 2010年2月 美国特拉华大学化学与生物系 访问学者
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支持扩展名:.rar .zip .doc .docx .pdf .jpg .png .jpeg长期以来从事耐药结核、自身免疫、代谢性疾病、恶性肿瘤等治疗领域的创新药物研发工作,自2002年起先后主持承担两项国家科技部“863”计划课题、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、四项国家新药创制科技重大专项课题、两项抗结核新药研发国际合作项目、多项企业委托新药研发项目,以及医科院医学与健康科技创新工程等课题。
近年来以通讯联系人发表SCI论文三十余篇,代表性论文如下:
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.
2. 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.
3. 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,* and Haihong Huang*. Discoveryof a Candidate Containing an(S)‑3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro‑1H‑inden Scaffold as aHighlyPotentPan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant forthe Treatment of Chronic Myeloid Leukemia. J.Med. Chem., 64,7434−7452.
4. Hui Chen, Bin Wang, PengLi, Hong Yan, Gang Li*, Haihong Huang*, Yu Lu,*. The optimization andcharacterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition. Bioorg.Med. Chem. Lett., 2021, 40, 127924.
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*, HaihongHuang*. 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.
6. 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.
7. 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.
8. Keli Cui, Meng Gao, Hongyi Zhao, Dongfeng Zhang*, Hong Yan* and Haihong Huang*. An Efficient Synthesis of Aryl-Substituted Pyrroles by the Suzuki–MiyauraCoupling Reaction of SEM-Protected Pyrroles. Molecules, 2019,24(8), 1594.
9. Meng Gao, Wenting Zhao, Hongyi Zhao, Ziyun Lin, Dongfeng Zhang* and Haihong Huang*. An efficientand facile access to highly functionalized pyrrole derivatives. BeilsteinJ. Org. Chem., 2018, 14, 884-890.
10. Peng-Xu Wang, Ya-NanWang, Zi-Yun Lin, Gang Li*, and Hai-Hong Huang*. Facile and efficientsynthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenationcondensation. Synthetic Communications, 2018, 48(10), 1183-1189.
11. Peng Li, Bin Wang, Xinwei Zhang, Sarah M. Batt, Gurdyal S. Besra, Tingting Zhang, Chen Ma, DongfengZhang, Ziyun Lin, Gang Li*, Haihong Huang*, Yu Lu*. Identification ofnovel 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, QianJiang, Ziyun Lin, Zhufang Shen*, Haihong Huang*. Discovery of novelxanthine 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. TetrahedronLetters, 2015, 56, 4683-4685.
15. Gang Li, Li Li, Haihong Huang* and Dali Yin*. Ti (IV)-catalyzed cascade synthesis oftetrahydrofuro[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 Da Li, CHEN Xiao Guang* & 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 Treatmentof Drug-Resistant Tuberculosis. J. Med. Chem., 2012, 55(19), 8409-8417.
专利:
获得20余项国内外专利授权
耐药结核、自身免疫、代谢性疾病、恶性肿瘤等治疗领域的创新药物研究,涉及药物分子设计与合成、活性天然产物的结构优化、新药研发项目的跨学科综合管理。
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