中国药科大学

徐云根，男，1964年7月生，药物化学专业博士，教授，博士生导师。现任药物化学教研室主任，江苏省药物设计与成药性优化重点实验室副主任，江苏省高校“青蓝工程”中青年学术带头人，江苏省第六届十大杰出专利发明人，江苏省高校优秀科技创新团队带头人。

近年来，专注于心脑血管、神经系统和抗肿瘤药物的设计与合成研究，先后获得候选药物2个。主持承担国家自然科学基金（No.30672512,No.81072520,NO.21272277,No.21472242）、国家重大新药创制科技重大专项（2009ZX09103-096、2015ZX09102001）等课题15余项。申请发明专利60余个，已获得授权专利30个，包括美国（US7820692、US7541355）、加拿大（CA2657355）、澳大利亚（AU2007276557）等外国专利6个；其中多个专利产品或技术已实施转让或产业化。先后主持开发并获得国家新药证书9本。在国内外核心刊物上发表论文90余篇，其中SCI论文50余篇。

研究方向：（1）新药分子设计与合成研究；（2）药物合成新技术与新工艺研究（硕士专业学位）。

联系方式：025-83271244；Email：xyg64@126.com

近三年发表的部分论文：

1.Qihua Zhu, Dezhong Ji, Tingting Liang, Xueyan Wang, Yungen Xu*. Efficient Palladium-Catalyzed C?H Fluorination of C(sp3)?H Bonds: Synthesis of β?Fluorinated Carboxylic Acids. Org Lett, 17, 3798?3801, 2015.

2.Zong-jie Gan, Yu-hua Wang, Yungen Xu*, Ting Guo, Jun Wang, Qiao Song, Xue-jun Xu, Shi-yuan Hu, Yu-jun Wang, De-chuan Wang, De-zhu Sun, Di Zhang, Tao Xi, Hao-dong Li, Hai-bo Zhang, Taijun Hang, Hong-guo Lu, Jing-gen Liu*. Discovery, Stereospecific Characterization and Peripheral Modification of 1-(Pyrrolidin-1-ylmethyl)-2-[(6-chloro-3- oxo-indan)-formyl]- 1,2,3,4-tetrahydroisoquinolines As Novel Selective k Opioid Receptor Agonists. Org Biomol Chem, 20(13), 5656-5673, 2015.

3.Shaochi Wang, Peng Dai, Yungen Xu*, Qiufang Chen, Qihua Zhu, Guoqing Gong*. Design, Synthesis, and Biological Evaluation of Dabigatran Etexilate Mimics, a Novel Class of Thrombin Inhibitors. Arch Pharm Chem. Life Sci, 348, 595–605, 2015.

4.Chen Zhou, Fangxia Zou, Yungen Xu*, Luyong Zhang, Xiaoming Zha*, Identification of New Non-steroidal TGR5 Agonists Using Virtual Screening with Combined Pharmacophore Models. Med Chem Res, 24(6):2561-2572,2015.

5.Chen Zhou, Di Kang, Yungen Xu*, Luyong Zhang, Xiaoming Zha*, Identification of Novel Selective LSD1 Inhibitors Using a Pharmacophore Based Virtual Screening Combined with Multiple Docking. Chem Biol Drug Design, 6：659-671, 2015.

6.Dong-Xing Chen, Jie Huang, Meng Liu, Yun-Gen Xu*, Cheng Jiang*. Design, Synthesis, and Evaluation of Non-ATP-Competitive Small-Molecule Polo-Like Kinase 1 (Plk1) Inhibitors. Arch Pharm Chem. Life Sci, 348(1):2–9, 2015.

7.Qiao Song,Dongmei Zhang, Qihua Zhu*, Yungen Xu*. p-Toluenesulfonohydrazide as Highly Efficient Initiator for Direct C?H Arylation of Unactivated Arenes. Org Lett, 16(20): 5272-5274, 2014.

8.Xiaobo Bao, Wei Yao, Qihua Zhu*, Yungen Xu*. Synthesis of 6-substituted phenanthridine derivatives by Palladium-Catalyzed Domino Suzuki-Miyaura/ Aza-Michael Reactions. Eur J Org Chem, (33):7443-7450, 2014.

9. Lei Shi*, Ting-Ting Wu, Zhi Wang, Jia-Yu Xue, Yun-Gen Xu*. Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. Eur J Med Chem, 84:698-707, 2014.

10.Yun Yang, Xinhui Wang, Qihua Zhu, Guoqing Gong*, Danmeng Luo, Aidou Jiang, Liyan Yang, Yungen Xu*. Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility. Bioorg Med Chem Lett, 24(7):1851-1855, 2014.

11.Jinyin Li, Jing Fang, Fanyi Zhong, Wenxue Li, Yuanjun Tang, Yungen Xu, Shilong Mao*, Guorong Fan*. Development and validation of a liquid chromatography/tandem mass spectrometry assay for the simultaneous determination of dabigatran etexilate, intermediate metabolite and dabigatran in 50 μL rat plasma and its application to pharmacokinetic study. Journal of Chromatography B. 973, 110–119, 2014.

12.Kun Liu, Shuowei Yao,Yinghan Lou, Yungen Xu*. Synthesis and anti-angiogenetic activity evaluation of N-(3-aryl acryloyl)aminosaccharide derivatives. Carbohyd Res, 381:83-92,2013.

13.Yan Tang, Zhewei Tu, Jing Sun, Xiong Zhu*, Kun Liu, Shuying He, Yungen Xu*. Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4. Lett Drug Des Discov,10(10): 935-941,2013.

14.QihuaZhu, XuyangWang, Zhaoxing Chu, Guangwei He*, Guangping Dong, YungenXu*. Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors. Bioorg Med Chem Lett, 23(7):1993-6,2013.

15.Yun-Zhan Li, Guo-Qing Gong*, Wen-Hui Yang, Xin-Hui Wang, Mei-Ling Jiang, Yi Zhou, Xiao-Zhi Yang, Yun-Gen Xu*, Guang-Wei He. Antithrombotic activity of HY023016, a novel Dabigatran prodrug evaluated in animal thrombosis models. Thrombosis Research, 131(5), 425-435,2013.

16.Haiping Zhou, Huiting Su, Zongjie Gan, Dechuan Wang, Yungen Xu*. An efficient procedure for synthesis of 2, 3-dihydro-1Hindene-1-methanamines. Res Chem Intermed, 39:4091-4098, 2013.

17.Zhi Wang, Yi-Qiao Fan, Lei Shi*, Yun-Gen Xu*. Synthesis, crystal structure, and biological activities of a Zn(II) complex with a Se substituted Schiff base. J Coord Chem, 66(11): 2032-2038, 2013.

18.Xiao-Zhi Yang, Xiao-Juan Diao, Wen-Hui Yang, Feng Li, Guang-Wei He, Guo-Qing Gong, Yun-Gen Xu*. Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate. Bioorg Med Chem Lett, 23: 2089-2092,2013.

19.Xu Zhang, Ting Peng, Xun Ji, Jian Li, Linjiang Tong, Zeng Li, Wei Yang, Yungen Xu, Mengyuan Li, Jian Ding, Hualiang Jiang, Hua Xie, Hong Liu*. Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. Bioorg Med Chem, 21(24):7988-7998, 2013.

20.Bin Hu, Qiao Song, Yungen Xu*. Scale-up Synthesis of Antidepressant Drug Vilazodone. Org Process Res Dev, 16(9):1552-1557,2012.

21.Xiao-Zhi Yang, Wen-Hui Yang, Yun-Gen Xu*, Xiao-Juan Diao, Guang-Wei He, Guo-Qing Gong*. Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity. Eur J Med Chem, 57: 21-28, 2012.

22.Yi Zhou, Guoqing Gong*, Wenhui Yang , Yin Wang, Jing Xu, Yungen Xu. The cardioprotective effect of TG-6, a newly synthesized compound, on ischemia-reperfusion injury in rats. Eur J Pharmacol, 683(1-3):190-196,2012.

23.靳璐, 姜向敏, 何广卫*, 徐文婷, 龚国清, 徐云根*. 4(6)-{2-[4-(2,3,4-三甲氧基苄基)哌嗪-1-基]-2-氧代乙氧基}芳甲酰胍类化合物的合成及其Na＋/H＋交换器-1抑制活性, 有机化学. 32(2): 326-332,2012.

24.Jin Ning, Yang Yun, Xu Wenting, Yang Xiaozhi, Gong Guoqing, Xu Yungen*. Synthesis and Bioactivity of Substituted Benzoylguanidine Derivatives as Potent Na+/H+ Exchanger Inhibitors. Chin J Chem, 30(2):333-340,2012.

25.Zongjie Gan, Bin Hu, Qiao Song, Yungen Xu*. Convenient Chlorination of Some Special Aromatic Compounds using N-Chlorosuccinimide. Synthesis-Stuttgart, 44(7):1074-1078,2012.

26.Qihua Zhu, Xuyan Wang, Yungen Xu*. Palladium-Catalyzed Tandem Reactions of β-(2-Bromophenyl)-α,β-Unsaturated Carbonyl Compounds with 2-Hydroxyphenylboronic Acid: A New Route to Benzo[c]chromenes. Eur J Org Chem, 6: 1112-1114, 2012.

出版的主要论著或教材：

1.《Medicinal Chemistry》(Second Edition)，科学出版社，2012年9月第二版，编者。

2.《药物化学》，中国医药科技出版社，2011年2月第二版，副主编。

3．国家执业药师资格考试应试指南《药学专业知识》（二），中国医药科技出版社，2011年1月第一版，编者。

4.《药物化学》，人民卫生出版社，2011年8月第七版，编者。

5.《药物化学实验方法学》，人民卫生出版社，2010年6月出版，编者。

6.《药物化学》，化学工业出版社，2015年8月出版，编者。

7.《药物化学实验与指导》（双语），中国医药科技出版社，2008年8月出版，副主编。

8.《药物设计学》，人民卫生出版社，2007年8月第一版，编者。