制药系
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古双喜,博士,教授,博士生导师

地址:湖北省武汉市东湖新技术开发区光谷一路206号59白菜网大化工楼

邮编:430205

QQ:64008556

Email:shuangxigu@163.com(更常用);sxgu@wit.edu.cn

课题组X-MOL网站:https://www.x-mol.com/groups/gu

教育背景

2008.09 – 2012.01,复旦大学化学系,有机化学,博士研究生

2003.09 – 2006.06,湖北省化学研究院,应用化学,硕士研究生

1999.09 – 2003.06,59论坛白菜专区化工系,化学工程与工艺,学士

工作履历

2012.02 – 目前,59白菜网,历任讲师/副教授/教授

2017.11-2018.10, University of Virginia, 访问学者

2014.10 – 2015.10,University of Virginia, 博士后

2006.07 – 2008.08,湖北省化学研究院,实习研究员

研究领域

(1)药物化学(抗HIV病毒、冠状病毒小分子药物)

Medicinal chemistry of anti-HIV and anti-coronavirus agents ;

(2)手性化学(手性分子荧光识别与分析、不对称合成与催化)

Chiral chemistry (Fluorescent recognition and analysis of chiral molecules, Asymmetric synthesis & catalysis)

(3)药物合成工艺 & 绿色化工过程

Synthetic process of pharmaceuticals, Green chemical process

学术成果

主持国家自然科学基金(3项)、武汉市国际科技合作项目、湖北省自然科学基金面上项目、湖北省自然科学基金青年基金、湖北省教育厅科学研究计划项目、湖北省高等学校青年教师深入企业行动计划项目、新农药创制与开发国家重点实验室开放基金等项目多项,主持多项企业委托的新药发现和原料药合成工艺开发项目。

以第一作者或通讯作者在Journal of the American Chemical Society、European Journal of Medicinal Chemistry、Bioorganic Chemistry、Chinese Chemical Letters、Organic Letters、Current Opinion in Pharmacology、Chemistry – A European Journal、Organic Process Research & Development、《药学学报》、《中国新药杂志》、《中国医药工业杂志》等期刊发表论文60余篇,其中1篇论文入选ESI高被引论文,3篇论文被遴选为封面论文,多项工作被ChemistryViews等亮点报道;受邀撰写多篇中、英文综述;多次受邀在国内外学术会议作学术报告;获得16项中国发明专利授权和1项湖北省科技成果登记证书;担任Journal of Medicinal Chemistry、Acta Pharmaceutica Sinica B、European Journal of Medicinal Chemistry、Organic Process Research & Development、Chemical Communications、Chinese Chemical Letters、《药学学报》、《中国医药工业杂志》等40余SCI期刊和中文核心期刊审稿人,多次获得优秀审稿人荣誉证书;2019年度获湖北省化学化工青年创新奖,2020年度获湖北省化学化工青年科学家论坛“青年报告最佳奖”,2021年获得2021 International Symposium of Frontier Sciences On New Drug Discovery(2021年国际药学前沿科学研讨会)优秀报告奖二等奖。

部分发表论文

[1] Ming, Wei; Lu, Wen-Long; Pannecouque, Christophe; Chen, Jiong; Wang, Hai-Feng; Xiao, Ya-Qi; Hu, Sha; Gu, Shuang-Xi*; Zhu, Yuan-Yuan*; Chen, Fen-Er.* Hybrids of delavirdine and piperdin-4-yl-aminopyrimidines (DPAPYs) as potent HIV-1 NNRTIs: Design, synthesis and biological activities. European Journal of Medicinal Chemistry, 2023, 248, 115114.

[2] Hu, Sha; Chen, Jiong; Cao, Jin-Xu; Zhang, Shuang-Shuang; Gu, Shuang-Xi*; Chen, Fen-Er*. Quinolines and isoquinolines as HIV-1 inhibitors: Chemical structures, action targets, and biological activities. Bioorganic Chemistry, 2023, 136, 106549.

[3] Li, Chenzong; Xiang, Xun; Zhang, Xianghe; He, Zhao-Lin*; Gu, Shuang-Xi*; Dong, Xiu-Qin*. Iridium-Catalyzed Intramolecular Asymmetric Allylation of Vinyl Benzoxazinones for the Synthesis of Chiral 4H-3,1-Benzoxazines via Kinetic Resolution. Organic Letters, 2023, 25, 1172−1177.

[4] Sun, Meng-Xin; Ni, Chuan-Zhi; Zhang, Fang-Qi; Zhu, Yuan-Yuan*; Zeng, Jie*; Gu, Shuang-Xi*. Chiral amino acid recognition in water: A BINOL-based fluorescent probe. Chinese Chemical Letters, 2023, 34, 108345.

[5] Jiang, Hanrui; Xiong, Huan; Gu, Shuang-Xi*; Wang, Mingliang*. E3 ligase ligand optimization of Clinical PROTACs. Frontiers in Chemistry, 2023, 11, 1098331.

[6] Chen, Jiong; Zhu, Yuan-Yuan*; Gu, Shuang-Xi*. Preparation of (S)-5,5ʹ,6,6ʹ,7,7ʹ,8,8ʹ- Octahydro-1,1'-bi-2-naphthol [(S)-H8BINOL]. Organic Syntheses, 2023, 100, 404-417.

[7] Hong, Yu; Zhu, Yuan-Yuan*; Gu, Shuang-Xi*. Preparation of (S)-3,3ʹ-Bis(1- pyrrolidinylmethyl)-5,5ʹ,6,6ʹ,7,7ʹ,8,8ʹ-octahydro-1,1'-bi-2-naphthol. Organic Syntheses, 2023, 100, 394–403.

[8] 李屈澳薇, 龚智华, 陈炯, 张双双, 古双喜*. 泼尼松磷酸酯二钠的合成及其在水中的溶解度测定. 中国药物化学杂志, 2023, 33(7), 529−534.

[9] Ming, Wei; Hu, Sha; Liu, Ye; Li, Qu-Ao-Wei; Zhu, Yuan-Yuan*; Gu, Shuang-Xi*. Recent Advances in the Chemical Synthesis of β-Nicotinamide Mononucleotide. Current Organic Chemistry, 2022, 26, 2151−2159.

[10] 刘烨, 明巍, 朱园园, 古双喜. 临床应用中的新型冠状病毒肺炎治疗药物研究进展. 中国新药杂志, 2022, 31(20), 2022−2028.

[11] Chen, Jiong; Ming, Wei; Fan, De-Hua; Gu, Shuang-Xi*. Synthesis and Characterization of Related Substances of Torasemide. Pharmaceutical Fronts, 2022, 4(3), e157−e161. (Cover feature)

[12] Gong, Zhihua; Hu, Sha; Jin, Xueping; Yu, Lei; Zhu, Yuanyuan; Gu, Shuangxi*. Synthetic Methods and Application of Phosphoester Prodrugs[J]. Progress in Chemistry, 2022, 34(9), 1972−1981

[13] Hong, Yu; Zhu, Yuan-Yuan; He, Qiuqin; Gu, Shuang-Xi*. Indole derivatives as tubulin polymerization inhibitors for the development of promising anticancer agents. Bioorganic & Medicinal Chemistry, 2022, 55, 116597.

[14] Ge, Rui; Zhu, YuanYuan; Wang, Haifeng; Gu, Shuang-Xi. Methods and Application of Absolute Configuration Assignment for Chiral Compounds. Chinese Journal of Organic Chemistry, 2022, 42(2), 424-433.

[15] 刘玉, 明巍, 李陈宗, 朱园园, 古双喜*. 拟肽类冠状病毒主蛋白酶抑制剂的研究进展. 药学学报, 2022, 57, 1977-1990.

[16] Wang, Yue; Gu, Shuang-Xi*; He, Qiuqin*; Fan, Renhua. Advances in the development of HIV integrase strand transfer inhibitors. European Journal of Medicinal Chemistry, 2021, 225, 113787.

[17] Liu, Ding; Zhu, Yuanyuan; Gu, Shuangxi*; Chen Fen-Er*. Application of Flow Chemistry in Halogenation. Chinese Journal of Organic Chemistry,2021, 41, 1002-1011.

[18] Gu, Shuang-Xi*; Zhu, Yuan-Yuan; Wang, Chao; Wang, Hai-Feng; Liu, Gen-Yan; Cao, Shuang; Huang, Lu. Recent discoveries in HIV-1 reverse transcriptase inhibitors. Current Opinion in Pharmacology, 2020, 54, 166-172.

[19] Xiao, Ting#; Tang, Jia-Fan#; Meng, Ge; Pannecouque, Christophe; Zhu, Yuan-Yuan; Liu, Gen-Yan; Xu, Zhi-Qiang; Wu, Feng-Shou; Gu, Shuang-Xi*; Chen, Fen-Er*. Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. European Journal of Medicinal Chemistry, 2020, 186, 111864.

[20] Wang, Chao; Liu, Xiao-Wen; Xiao, Ting; Xu, Zhi-Qiang; Cao, Shuang; Wang, Hai-Feng; Yan, Qiong-Jiao; Gu, Shuang-Xi*; Zhu, Yuan-Yuan*. Anticancer activity evaluation of indazolyl-substituted piperidin-4-yl-aminopyrimidines. Medicinal Chemistry Research, 2020, 29(5), 910-915.

[21] Wang, Haifeng*; Sun, Xiangli; Hu, Manman; Zhang, Xiaoyi; Xie, Lele; Gu, Shuangxi*. Bromination of α-Diazo Phenylacetate Derivatives Using Cobalt(II) Bromide. Advanced Synthesis & Catalysis, 2020, 362(16), 3347-3351.

[22] Gu, Shuang-Xi; Wang, Hai-Feng; Zhu, Yuan-Yuan; Chen, Fen-Er. Natural Occurrence, Biological Functions, and Analysis of D-Amino Acids. Pharmaceutical Fronts, 2020, 2(2): e79-e87. (Cover feature)

[23] Zhu, Yuan-Yuan; Wu, Xue-Dan; Gu, Shuang-Xi*; Pu, Lin*. Free Amino Acid Recognition: A Bisbinaphthyl-Based Fluorescent Probe with High Enantioselectivity. Journal of the American Chemical Society, 2019, 141(1): 175-181. (ESI Highly cited paper);https://www.x-mol.com/news/15900

[24] Zhu, Yuan-Yuan; Wu, Xue-Dan; Abed, Mehdi; Gu, Shuang-Xi*; Pu, Lin*. Biphasic Enantioselective Fluorescent Recognition of Amino Acids by a Fluorophilic Probe. Chemistry – A European Journal, 2019, 25(33): 7866-7873. (Hot paper and cover feature article of Chem. Eur. J., Highlighted by ChemistryViews);https://www.chemistryviews.org/details/news/11157496/Enantioselective_Recognition_of_Amino_Acids.html;https://www.x-mol.com/news/18278

[25] Gu, Shuang-Xi*; Xiao, Ting; Zhu, Yuan-Yuan; Liu, Gen-Yan; Chen, Fen-Er*. Recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket. European Journal of Medicinal Chemistry, 2019, 174: 277-291.

[26] Gu, Shuang-Xi*; Lu, Huan-Huan; Liu, Gen-Yan; Ju, Xiu-Lian; Zhu, Yuan-Yuan*. Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors. European Journal of Medicinal Chemistry, 2018, 158: 371-392.

[27] Liu, Genyan*; Wan, Youlan; Wang, Wenjie; Fang, Sai; Gu, Shuangxi*; Ju, Xiulian. Docking-based 3D-QSAR and pharmacophore studies on diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. Molecular Diversity, 2019, 23: 107-121.

[28] Liu, Genyan*; Wang, Wenjie; Wan, Youlan; Ju, Xiulian; Gu, Shuangxi*. Application of 3D-QSAR, Pharmacophore, and Molecular Docking in the Molecular Design of Diarylpyrimidine Derivatives as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors. International Journal of Molecular Sciences, 2018, 19(5): 1436.

[29] Lu, Huan-Huan; Xue, Ping; Zhu, Yuan-Yuan*; Ju, Xiu-Lian; Zheng, Xiao-Jiao; Zhang, Xun; Xiao, Ting; Pannecouque, Christophe*; Li, Ting-Ting; Gu, Shuang-Xi*. Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. Bioorganic & Medicinal Chemistry, 2017, 25(8): 2491-2497.

[30] Xue, Ping; Lu, Huan-Huan; Zhu, Yuan-Yuan*; Ju, Xiu-Lian; Pannecouque, Christophe; Zheng, Xiao-Jiao; Liu, Gen-Yan; Zhang, Xiu-Lan; Gu, Shuang-Xi*. Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. Bioorganic & Medicinal Chemistry Letters, 2017, 27(8): 1640-1643.

[31] 张旬, 古双喜*, 肖婷, 朱园园, 巨修练. 富马酸喹硫平的合成研究进展. 中国医药工业杂志, 2017, 48(10): 1409-1423.

[32] Gu, Shuang-Xi*; Xue, Ping; Ju, Xiu-Lian; Zhu, Yuan-Yuan*. Advances in rationally designed dual inhibitors of HIV-1 reverse transcriptase and integrase. Bioorganic & Medicinal Chemistry, 2016, 24(21): 5007-5016.

[33] Gu, Shuang-Xi*; Qiao, Heng; Zhu, Yuan-Yuan; Shu, Qi-Chao; Liu, Hui; Ju, Xiu-Lian*; De Clercq, Erik; Balzarini, Jan; Pannecouque, Christophe. A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. Bioorganic & Medicinal Chemistry, 2015, 23(20): 6587-6593.

[34] Gu, Shuang-Xi*; Zhu, Yuan-Yuan; Chen, Fen-Er*; De Clercq, Erik; Balzarini, Jan; Pannecouque, Christophe. Structural modification of diarylpyrimidine derivatives as HIV-1 reverse transcriptase inhibitors. Medicinal Chemistry Research, 2015, 24(1): 220-225.

[35] Gu, Shuang-Xi; Huang, Wen-Cai; Wu, Xue-Dan; Ying, Jun; Pu, Lin*. Simple and Efficient One-Step Synthesis of a Highly Enantioselective Catalyst 3,3′-Di(pyrrolidinylmethyl)- H8BINOL. Synthetic Communications, 2015, 45(13): 1541-1545.

[36] Gu, Shuang-Xi; Du, Jia-Wen; Ju, Xiu-Lian*; Chen, Qing-Ping. A Scalable One-Pot Process for the Synthesis of Florfenicol Phosphodiester. Organic Process Research & Development, 2014, 18(4): 552-554.

[37] Gu, Shuang-Xi; Li, Zhi-Ming; Ma, Xiao-Dong.; Yang, Shi-Qiong; He, Qiu-Qin*; Chen, Fen-Er*; De Clercq, Erik; Balzarini, Jan; Pannecouque, Christophe. Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. European Journal of Medicinal Chemistry, 2012, 53: 229-234.

[38] Gu, Shuang-Xi; Yang, Shi-Qiong; He, Qiu-Qin; Ma, Xiao-Dong; Chen, Fen-Er*; Dai, Hui-Fang*; Clercq, Erik De; Balzarini, Jan; Pannecouque, Christophe. Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. Bioorganic & Medicinal Chemistry, 2011, 19(23): 7093-7099.

[39] Gu, Shuang-Xi.; He, Qiu-Qin; Yang, Shi-Qiong; Ma, Xiao-Dong; Chen, Fen-Er*; De Clercq, Eric; Balzarini, Jan; Pannecouque, Christophe. Synthesis and structure-activity relationship of novel diarylpyrimidines with hydroxymethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. Bioorganic & Medicinal Chemistry, 2011, 19(17): 5117-5124.

[40] Gu, Shuang-Xi; Zhang, Xuan; He, Qiu-Qin; Yang, Liu-Meng; Ma, Xiao-Dong; Zheng, Yong-Tang; Yang, Shi-Qiong; Chen, Fen-Er*. Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors. Bioorganic & Medicinal Chemistry, 2011, 19(14): 4220-4226.

参编专著

Privileged Scaffolds in Drug Discovery》Chapter 23, 2023, Elsevier Academic Press.

授权专利

获批授权中国发明专利14件。

ZL202210261337.2,吲哚哌啶嘧啶类衍生物在制备新型冠状病毒抑制剂中的应用;

ZL202210247140.3,吲哚哌啶嘧啶类衍生物及其制备方法和用途;

ZL202210802669.7,一种雌二醇磷酸酯及其盐的制备方法和应用;

ZL202210802691.1,一种泼尼松磷酸酯及其盐的制备方法和应用;

ZL202210802483.1,一种雌酮磷酸酯及其盐的制备方法和应用;

ZL202210671057.9,一种含有全氟烷基的手性荧光探针及其制备方法和应用;

ZL202210665107.2,一种具有苯并噻唑基团的手性荧光探针及其制备和应用;

ZL201910698458.1,一种吲唑哌啶嘧啶类衍生物及其制备方法和用途;

ZL201910811980.6,一种吲唑哌啶嘧啶类化合物的应用;

ZL201710108100.X,二芳基嘧啶‑二酮酸类杂合型HIV‑1抑制剂及其制备方法;

ZL201510516039.3,一种二芳基嘧啶类HIV‑1抑制剂及其制备方法;

ZL201410798040.5,5-(4-硝基苯基)-3-羟基异噁唑及其制备工艺和用途;

ZL201310136496.0,氟苯尼考磷酸二酯及盐及其制备方法;

ZL201310697748.7,托曲珠利碱金属盐及其制备方法和用途。

成果登记证书

作为骨干人员开发的“氟苯尼考磷酸二酯合成及小试工艺研究”已于2014年12月获湖北省科技成果登记证书

科研项目

1)主持项目:主持国家自然科学基金面上项目、国家自然科学基金青年基金、武汉市国际科技合作项目、湖北省自然科学基金青年基金、湖北省自然科学基金面上项目、湖北省教育厅科学研究计划项目、湖北省高等学校青年教师深入企业行动计划项目、药物制备关键技术教育部重点实验室、新农药创制与开发国家重点实验室开放基金各一项,并主持多项原料药合成工艺开发项目。

2)参与项目:国家自然科学基金面上项目、国家自然科学基金青年基金和多项企业委托工艺开发项目等。

学术兼职

受聘为国家自然科学基金评审专家、湖北省科技经济融合学会副秘书长、湖北省科技领军人才促进会理事、湖北省科学技术厅权威专家库高端专家、教育部学位与研究生教育发展中心学位论文评审专家、国家药品监督管理局药物制剂质量研究与控制重点实验室学术委员会委员等,担任2020年度湖北省院士专家企业行成员、2021年度湖北省中小微企业科技副总、湖北省科技领军人才发展促进会会员、中国化工学会会员、中国化学会会员等。

担任《Mini-Reviews in Medicinal Chemistry》编委、《Chinese Chemical Letters》青年编委、《中国医药工业杂志》编委、《合成化学》编委、《Green Synthesis & Catalysis》青年编委、《Pharmaceutical Fronts》青年编委、《59论坛白菜专区学报》编委等职;担任多个中英文刊的专刊客座编辑;担任Journal of Medicinal Chemistry、Acta Pharmaceutica Sinica B、European Journal of Medicinal Chemistry、Organic Process Research & Development、Chemical Communications、Chinese Chemical Letters、《药学学报》、《中国医药工业杂志》等40余SCI期刊和中文核心期刊审稿人。

奖励与荣誉

湖北省优秀科技论文(2021-2023);

湖北省高等学校教学成果奖一等奖(2018),二等奖(2023);

Pharmaceutical Fronts 2021-2023优秀组稿奖;

59论坛白菜专区优秀研究生学位论文指导老师(明巍、胡莎、肖婷、薛萍、卢欢欢);

2021 International Symposium of Frontier Sciences On New Drug Discovery(2021年国际药学前沿科学研讨会)优秀报告奖二等奖;

2021-2023年连续三年获得“优秀班主任;

武汉知识产权研究会2020年度征文三等奖;

2020年度获Chinese Chemical Letters优秀审稿人;

2020年度获湖北省化学化工青年科学家论坛“青年报告最佳奖”;

2019年度获湖北省化学化工青年创新奖;

2017-2020年度59论坛白菜专区先进工作者;

2019-2020年度59论坛白菜专区优秀导师;

2017-2019年度59论坛白菜专区优秀共产党员;

2019年度获得多项Certificate of Outstanding Contribution in Reviewing荣誉证书(Elsevier);湖北省第十届老员工化学(化工)学术创新成果报告会一等奖指导老师,2017年;

指导的两名研究生薛萍、卢欢欢同时获得59论坛白菜专区“优秀毕业研究生”荣誉称号;

教研论文获第四届中国石油和化工教育科学研究成果奖论文三等奖,2016年,排名第一;指导的陈佳同学学士学位论文获得湖北省优秀学士学位论文,2016年,指导老师;

指导的夏甜甜、洪彩华、徐侃、余小晶、柴智、费华丽同学荣获第六届“国药工程杯”全国老员工制药工程设计竞赛一等奖,2016年,指导老师;

指导的刘家密同学获得“海普瑞杯”第六届全国员工制药工程研究征文比赛二等奖,2016年,指导老师;

指导的刘家密、余小晶、单艳超同学湖北省第九届老员工化学(化工)学术创新成果报告会三等奖,2016年,指导老师;

指导的刘忱同学获湖北省第八届老员工化学(化工)学术创新成果报告会三等奖,2015年,指导老师;

指导的薛萍同学获“海普瑞杯”第五届全国员工制药工程研究征文比赛三等奖,2015年,指导老师;

2014年获评59论坛白菜专区先进科技工作者;

指导的徐丹同学获“东富龙杯”第三届全国员工制药工程研究征文比赛三等奖,2013年,指导老师。

指导的段婷、万雯、朱海游同学获湖北省第六届老员工化学(化工)学术创新成果报告会二等奖,2013,指导老师;

指导的李牡林同学获“东富龙杯”第三届全国员工制药工程研究征文比赛优胜奖,2012年,指导老师;

指导的徐丹同学获“东富龙杯”第三届全国员工制药工程研究征文比赛三等奖,2013年,指导老师;

全国手性物质科学暑期学校(教育部主办、国家自然科学基金委资助)优秀学员证书,2012年。

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