天然化合物的构效关系研究，有机化学

   

070303-有机化学

天然化合物的构效关系，抗病毒活性研究

2008-09--2011-12   中国科学院新疆理化技术研究所   博士
2004-09--2007-07   南开大学   硕士
2000-09--2004-07   忻州师范学院   本科

研究生学历

博士学位

   

2014-10~现在, 中国科学院新疆理化技术研究所, 副研究员
2012-03~2014-09,中国科学院新疆理化技术研究所, 助理研究员
2007-09~2008-07,新疆科技学校, 教师

   

（1） 第十三届新疆自然科学优秀学术论文, 一等奖, 省级, 2014
（2） 第十二届新疆自然科学优秀学术论文, 二等奖, 省级, 2012

（ 1 ） 一枝蒿酮酸糖酯类衍生物及其制备方法和用途, 发明, 2012, 第 2 作者, 专利号: ZL201010191025.6
（ 2 ） 含哌嗪环的一枝蒿酮酸酯类衍生物及其制备方法和用途, 发明, 2013, 第 2 作者, 专利号: ZL201010227465.2
（ 3 ） 一枝蒿酮酸异恶唑酰胺类衍生物及其制备方法和用途, 发明, 2013, 第 2 作者, 专利号: ZL201110213499.0
（ 4 ） 一枝蒿酮酸酯类衍生物及其制备方法和用途, 发明, 2014, 第 2 作者, 专利号: ZL201110213512.2
（ 5 ） 一枝蒿酮酸含杂环酰胺类衍生物及其制备方法和用途, 发明, 2016, 第 3 作者, 专利号: ZL201310039406.6
（ 6 ） 一枝蒿酮酸含杂环酯类衍生物及其制备方法和用途, 发明, 2016, 第 4 作者, 专利号: ZL201310039407.0
（ 7 ） 一枝蒿酮酸含杂环和糖的酯类衍生物及其制备方法和用途, 发明, 2016, 第 4 作者, 专利号: ZL201310219905.3
（ 8 ） 一种2,5-二氨基-3,4-噻吩二羧酸乙酯衍生物的制备方法和用途, 发明, 2016, 第 3 作者, 专利号: ZL201410302424.3
（ 9 ） 异叶青兰有效部位的制备方法和用途, 发明, 2014, 第 5 作者, 专利号: ZL201310031267.2
（ 10 ） 一枝蒿酮酸含杂环和糖的酰胺类衍生物及其制备方法和用途, 发明, 2016, 第 3 作者, 专利号: ZL201310248785.X

   

[1] 1.\tRuqi Xi, Rahima Abdulla, jiangyu zhao, Haji Akber Aisa, Yongqiang Liu. Pharmacokinetic study and metabolite identification of CAM106 in rats by validated UHPLC-MS/MS. Pharmaceuticals[J]. 2023, 16: 728-, https://www.mdpi.com/1424-8247/16/5/728/html.
[2] Song, Buer, Nie, Lifei, Bozorov, Khurshed, Niu, Chao, Kuryazov, Rustamkhon, Akber Aisa, Haji, Zhao, Jiangyu. Furo2,3-dpyrimidines as Mackinazolinone/Isaindigotone Analogs: Synthesis, Modification, Antitumor Activity, and Molecular Docking Study. CHEMISTRY & BIODIVERSITY. 2023, http://dx.doi.org/10.1002/cbdv.202201059.
[3] 张维舒, 聂礼飞, Khurshed Bozorov, 阿吉艾克拜尔·艾萨, 赵江瑜. 2，5-二氨基噻吩-3，4-二羧酸二乙酯衍生物的合成及抗肿瘤活性研究. 有机化学[J]. 2023, 43: [4] 刘奇, 聂礼飞, BOZOROV, Khurshed, 赵江瑜. 1，2，3-三氮唑并4，5-d嘧啶酮三环类衍生物的合成及抗肿瘤活性研究. 中国药物化学杂志[J]. 2021, 31(12): 945-954, http://lib.cqvip.com/Qikan/Article/Detail?id=7106461540.
[5] Ablajan, Nurfida, Zhao, Bo, Zhao, JiangYu, Wang, BianLin, Sagdullaev, Sh Sh, Aisa, H A. Diterpenoid alkaloids from Aconitum barbatum var. puberulum Ledeb. PHYTOCHEMISTRY[J]. 2021, 181(1): http://dx.doi.org/10.1016/j.phytochem.2020.112567.
[6] Zhao, Bo, Ablajan, Nurfida, Zhao, JiangYu, Kodirova, D R, Sagdullaev, Sh Sh, Aisa, H A. Two new C-19-diterpenoid alkaloids from Aconitum smirnovii. PHYTOCHEMISTRY LETTERS[J]. 2020, 38(8): 96-100, http://dx.doi.org/10.1016/j.phytol.2020.05.007.
[7] Yuan, WenJuan, Gao, WenFen, Zhao, JiangYu, Zhang, Yu, Chen, DuoZhi, Li, ShunLin, Di, YingTong, Hao, XiaoJiang. Diterpenes with potential treatment of vitiligo from the aerials parts of Euphorbia antiquorum L. FITOTERAPIA[J]. 2020, 144(7): http://ir.kib.ac.cn/handle/151853/72049, http://www.irgrid.ac.cn/handle/1471x/6927915, http://ir.kib.ac.cn/handle/151853/72050, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000537596000004&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=3a85505900f77cc629623c3f2907beab.
[8] Li, Gen, Obul, Mamateli, Zhao, Jiangyu, Liu, Geyu, Lu, Wei, Aisa, Haji Akber. Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2019, 29(19): http://dx.doi.org/10.1016/j.bmcl.2019.08.009.
[9] Xue, WenJuan, Zhao, Bo, Zhao, JiangYu, Sagdullaev, Sh Sh, Aisa, Haji Akber. Three new diterpenoid alkaloids from Delphinium naviculare var. lasiocarpum W. T. Wang. PHYTOCHEMISTRY LETTERS[J]. 2019, 33: 12-16, http://dx.doi.org/10.1016/j.phytol.2019.06.009.
[10] Bozorov, Khurshed, Zhao, Jiangyu, Aisa, Haji A. 1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview. BIOORGANIC & MEDICINAL CHEMISTRY[J]. 2019, 27(16): 3511-3531, http://dx.doi.org/10.1016/j.bmc.2019.07.005.
[11] Obul, Mamateli, Wang, Xincheng, Zhao, Jiangyu, Li, Gen, Aisa, Haji Akber, Huang, Guozheng. Structural modification on rupestonic acid leads to highly potent inhibitors against influenza virus. MOLECULAR DIVERSITY[J]. 2019, 23(1): 1-9, https://www.webofscience.com/wos/woscc/full-record/WOS:000459517700001.
[12] Nasrullaev, Azizbek, Bozorov, Khurshed, Bobakulov, Khayrulla, Zhao, Jiangyu, Nie, Li Fei, Turgunov, Kambarali K, Elmuradov, Burkhon, Aisa, Haji A. Synthesis, characterization, and antimicrobial activity of novel hydrazone-bearing tricyclic quinazolines. RESEARCH ON CHEMICAL INTERMEDIATES[J]. 2019, 45(4): 2287-2300, http://ir.xjipc.cas.cn/handle/365002/5705.
[13] 黄国正. Diversity-oriented synthesis of amide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones and evaluation their influence on melanin synthesis in murine B16 cells. Heterocyclic Communications. 2018, [14] Nie, Li Fei, Bozorov, Khurshed, Huang, Guozheng, Zhao, Jiangyu, Niu, Chao, Aisa, Haji Akber. Design, synthesis, and toward a side-ring optimization of tricyclic thieno2,3-dpyrimidin-4(3H)-ones and their effect on melanin synthesis in murine B16 cells. PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS[J]. 2018, 193(10): 656-667, https://www.webofscience.com/wos/woscc/full-record/WOS:000457566000006.
[15] Yusuf, Abdullah, Zhao, Jiangyu, Wang, Bianlin, Aibibula, Paruke, Aisa, Haji Akber, Huang, Guozheng. Total synthesis of rupestine G and its epimers. ROYAL SOCIETY OPEN SCIENCE[J]. 2018, 5(3): http://ir.xjipc.cas.cn/handle/365002/5791.
[16] Nie, Li Fei, Huang, Guozheng, Bozorov, Khurshed, Zhao, Jiangyu, Niu, Chao, Sagdullaev, Shamansur S, Aisa, Haji A. Diversity-oriented synthesis of amide derivatives of tricyclic thieno2,3-d pyrimidin-4(3H)-ones and evaluation of their influence on melanin synthesis in murine B16 cells (vol 24, pg 43, 2018). HETEROCYCLIC COMMUNICATIONSnull. 2018, 24(4): 241-241, https://www.webofscience.com/wos/woscc/full-record/WOS:000440655800011.
[17] Zhao, B, Zhao, J Y, Sagdullaev, Sh Sh, Aisa, H A. DITERPENE ALKALOIDS FROM Aconitum smirnovii. CHEMISTRY OF NATURAL COMPOUNDS[J]. 2018, 54(4): 828-830, https://www.webofscience.com/wos/woscc/full-record/WOS:000440423000060.
[18] Ablajan, Nurfida, Zhao, Bo, Xue, Wenjuan, Ruzi, Zukela, Zhao, Jiangyu, Aisa, Haji Akber. Diterpenoid Alkaloids from Delphinium aemulans. NATURAL PRODUCT COMMUNICATIONS[J]. 2018, 13(11): 1429-1431, https://www.webofscience.com/wos/woscc/full-record/WOS:000456230000004.
[19] Xue, WenJuan, Zhao, Bo, Ruzi, Zukela, Zhao, JiangYu, Aisa, Haji Akber. Norditerpenoid alkaloids from Delphinium pseudoaemulans C. Y. Yang et B. Wang. PHYTOCHEMISTRY[J]. 2018, 156: 234-240, http://dx.doi.org/10.1016/j.phytochem.2018.09.010.
[20] Li, Gen, Zhao, JiangYu, Niu, Chao, Nie, LiFei, Dong, ChangZhi, Aisa, Haji Akber. Structure-activity relationship studies of 1-(1 '-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2017, 27(6): 1484-1487, http://dx.doi.org/10.1016/j.bmcl.2016.06.011.
[21] Bozorov, Khurshed, Zhao, Jiang Yu, Nie, Li Fei, Ma, HaiRong, Bobakulov, Khayrulla, Hu, Rui, Rustamova, Nigora, Huang, Guozheng, Efferth, Thomas, Aisa, Haji A. Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and antiinfluenza virus agents. Part. RSC ADVANCES[J]. 2017, 7(50): 31417-31427, http://dx.doi.org/10.1039/c7ra04808d.
[22] Zhao Jiangyu. Structure–activity relationship studies of 1-(10-hydroxyalkyl) rupestonic acid methyl esters against influenza viruses. Bioorganic & Medicinal Chemistry Letters. 2017, [23] Bozorov, Khurshed, Nie, Li Fei, Zhao, Jiangyu, Aisa, Haji A. 2-Aminothiophene scaffolds: Diverse biological and pharmacological attributes in medicinal chemistry. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRYnull. 2017, 140: 465-493, http://dx.doi.org/10.1016/j.ejmech.2017.09.039.
[24] Zhao, Jiangyu, Niu, Chao, Li, Gen, Aisa, Haji Akber. Synthesis of Rupestonic Acid Derivatives with Antiviral Activity. CHEMISTRY OF NATURAL COMPOUNDS[J]. 2017, 53(2): 276-283, http://ir.xjipc.cas.cn/handle/365002/4783.
[25] Khurshed Bozorov, JiangYu Zhao, Haji A Aisa. Recent advances in ipso-nitration reactions. ARKIVOC[J]. 2016, 41-66, https://doi.org/10.24820/ark.5550190.p009.852.
[26] Niu, Chao, Yin, Li, Nie, Li Fei, Dou, Jun, Zhao, Jiang Yu, Li, Gen, Aisa, Haji Aker. Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo. BIOORGANIC & MEDICINAL CHEMISTRY[J]. 2016, 24(21): 5440-5448, http://dx.doi.org/10.1016/j.bmc.2016.08.066.
[27] Ma, LinLin, Wang, HuiQiang, Wu, Ping, Hu, Jin, Yin, JinQiu, Wu, Shuo, Ge, Miao, Sun, WenFang, Zhao, JiangYu, Aisa, Haji Akber, Li, YuHuan, Jiang, JianDoug. Rupestonic acid derivative YZH-106 suppresses influenza virus replication by activation of heme oxygenase-1-mediated interferon response. FREE RADICAL BIOLOGY AND MEDICINE[J]. 2016, 96(7): 347-361, http://dx.doi.org/10.1016/j.freeradbiomed.2016.04.021.
[28] Bozorov, Khurshed, Zhao, JiangYu, Elmuradov, Burkhon, Pataer, Apar, Aisa, Haji A. Recent developments regarding the use of thieno2,3-dpyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2015, 102(9): 552-573, http://dx.doi.org/10.1016/j.ejmech.2015.08.018.
[29] Gu, Dongyu, Yang, Yi, Chen, Qibin, Habasi, Madina, Zhao, Jiangyu, Aisa, Haji Akber. Identification of metabolites of rupestonic acid in rat urine by liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry. BIOMEDICAL CHROMATOGRAPHY[J]. 2015, 29(4): 595-603, https://www.webofscience.com/wos/woscc/full-record/WOS:000352094800016.
[30] He, YaoWu, Dong, ChangZhi, Zhao, JiangYu, Ma, LinLin, Li, YuHuan, Aisa, Haji Akber. 1,2,3-Triazole-containing derivatives of rupestonic acid: Click-chemical synthesis and antiviral activities against influenza viruses. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2014, 76(4): 245-255, http://dx.doi.org/10.1016/j.ejmech.2014.02.029.
[31] Bozorov, Khurshed, Ma, HaiRong, Zhao, JiangYu, Zhao, HaiQing, Chen, Hua, Bobakulov, Khayrulla, Xin, XueLei, Elmuradov, Burkhon, Shakhidoyatov, Khusnutdin, Aisa, Haji A. Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2014, 84(9): 739-745, http://dx.doi.org/10.1016/j.ejmech.2014.07.065.
[32] 赵江瑜, 阿吉艾克拜尔艾萨. 新型一枝蒿酮酸异噁唑衍生物的合成及其抗A，B型流感病毒活性研究. 有机化学[J]. 2012, 32(2): 333-337, http://lib.cqvip.com/Qikan/Article/Detail?id=40979431.
[33] Zhao, Jiangyu, Aisa, Haji Akber. Synthesis and anti-influenza activity of aminoalkyl rupestonates. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2012, 22(6): 2321-2325, http://dx.doi.org/10.1016/j.bmcl.2012.01.056.
[34] Zhao, Jiangyu, Aisa, Haji Akber. Synthesis of Novel Isoxazole Contained Rupestonic Acid Derivatives and in vitro Inhibitory Activity against Influenza Viruses A and B. CHINESE JOURNAL OF ORGANIC CHEMISTRY[J]. 2012, 32(2): 333-337, http://dx.doi.org/10.6023/cjoc1108081.
[35] 雍建平, 赵江瑜, 阿吉艾克拜尔艾萨. 3-脱氧一枝蒿酮酸的合成及体外抗流感病毒活性研究. 时珍国医国药[J]. 2011, 22(1): 19-21, http://lib.cqvip.com/Qikan/Article/Detail?id=39835790.
[36] Sun, Huailin, Zhang, Han, Liu, Qiuhua, Yu, Lei, Zhao, Jiangyu. Metal-catalyzed copolymerization of imines and CO: A non-amino acid route to polypeptides. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION[J]. 2007, 46(32): 6068-6072, https://www.webofscience.com/wos/woscc/full-record/WOS:000248931100006.
[37] 赵明根, 石玉芳, 赵江瑜, 吕海斌, 张婷婷. 1-吡啶甲酰基-4-烯丙基氨基硫脲的合成与结构表征. 山西大学学报：自然科学版[J]. 2007, 30(1): 64-67, http://lib.cqvip.com/Qikan/Article/Detail?id=24610060.

   

（ 1 ） 一枝蒿酮酸衍生物的合成及初步的抗流感病毒药效学研究, 主持, 国家级, 2015-01--2017-12
（ 2 ） 中国科学院青年创新促进会成员, 主持, 部委级, 2015-01--2018-12
（ 3 ） 一枝蒿碱的全合成及衍生物的抗流感病毒活性研究, 主持, 省级, 2015-01--2017-12
（ 4 ） 栽培植物汇总C20二萜类生物碱的分离纯化及活性研究, 主持, 国家级, 2017-01--2018-12
（ 5 ） 一枝蒿酮酸衍生物的抗病毒活性及构效关系研究, 主持, 部委级, 2012-09--2016-08
（ 6 ） 中国科学院中亚药物研发中心, 参与, 部委级, 2013-01--2020-12
（ 7 ） 中亚干旱区天然产物研究, 主持, 部委级, 2016-01--2020-12
（ 8 ） 一枝蒿酮酸衍生物的成药性研究, 参与, 省级, 2013-01--2015-12
（ 9 ） 一枝蒿酮酸衍生物的合成及生物活性研究, 参与, 省级, 2009-06--2011-12
（ 10 ） 维药一枝蒿抗病毒药效及其代谢研究, 参与, 国家级, 2012-01--2014-12
（ 11 ） 靶向Pgp肿瘤MDR逆转剂个性化先导化合物的发现研究, 参与, 部委级, 2018-01--2019-12

现指导学生

陈磊  硕士研究生  070303-有机化学