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成果及论文

代表性论文(药物化学方向)

1.      Liu Sisi, # Ma Congxuan, # Quan Zhengyang, Ding Jing, Yang Liang, Liu Simeng, Zhang Heao, Qing Hong *, Liang Jian-Hua *. Discovery of Novel diphenyl acrylonitrile derivatives that Promote Adult Rats’ Hippocampal Neurogenesis. International Journal of Molecular Sciences, 2024, 25(2), 1241

2.      Yuan Feiyan, Ding Jing, Sun Yiyang, Liang Jianhua, Luo Yunzi, Yu Yang*. Synthesis of Trifluoromethylated Monoterpenes by an Engineered Cytochrome P450. Chemistry-A European Journal, 2024, 30(10):e202302936

3.      Feng Zi-Qiang, # Ding Jing, # Zhu Min-Zhen, # Xie Wei-Song, Liu Rui-Chen, Liu Si-Si, Liu Si-Meng, Yu Ming-Jia, * Zhu Xin-Hong * Liang Jian-Hua *. Discovery of a novel lead characterized by a stilbene-extended scaffold against sepsis as soluble epoxide hydrolase inhibitors. European Journal of Medicinal Chemistry, 2024, 266, 116113

4.      Shehzadi Kiran, Yu Mingjia*, Liang Jianhua*. De Novo Potent Peptide Nucleic Acid Antisense Oligomer Inhibitors Targeting SARS-CoV-2 RNA-Dependent RNA Polymerase via Structure-Guided Drug Design. International Journal of Molecular Sciences, 2023, 24(24), 17473

5.      Shehzadi Kiran, Saba Afsheen, Yu Mingjia*, Liang Jianhua*. Structure-Based Drug Design of RdRp Inhibitors against SARS-CoV-2. Topics in Current Chemistry, 2023, 381(5):22

6.      Lian Xiaotian, Liu Wentian, Fan Bingzhi, Yu Mingjia* and Liang Jianhua*. Design, Synthesis and Biological Evaluation of Conjugates of 3-O-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains. Molecules, 2023, 28(3), 1327

7.      刘兴周, 于明加*, 梁建华*. 原小檗碱骨架的合成及其抗炎活性研究进展. 有机化学, 2023, 43, 1325-1340

8.      Xie Wei-Song, Shehzadi Kiran, * Ma Hong-Le, Liang Jian-Hua.* A Potential Strategy for Treatment of Neurodegenerative Disorder by Regulation of Adult Hippocampal Neurogenesis in Human Brain. Current Medicinal Chemistry. 2022, 29(32)5315-5347

9.      Liu Xie-Peng, Lv Wei, Zhao Fei, Ding Jing, Zhang Jue-Ru, Xue Feng, Zhang Jian-Zhong, Liu Li-Yong, Cushman Mark, Li Yun,* Liang Jian-Hua *. Design and Synthesis of Novel Macrolones Bridged with Linkers from 11,12-Positions of Macrolides. Bioorganic & Medicinal Chemistry Letters, 2022, 68: 128761

10.  Zhang Wen#, Li ZhiFei #, Sun Yufan#, Cui Peng#, Liang Jianhua, Xing Qinghe, Wu Jing, Xu Yanhui, Zhang Wenhong, Zhang Ying, He Lin, Gao Ning*. Cryo-EM structure of Mycobacterium tuberculosis 50S ribosomal subunit bound with clarithromycin reveals dynamic and specific interactions with macrolides. Emerging Microbes & Infections, 2022, 11(1): 293-305

11.  Zhang Heao, Xiang Lin, Yang Liang, Wu Si, Liu Sisi, Zhao Juan, Song Da, Ma Congxuan, Ni Junjun, Quan Zhenzhen, Liang Jianhua*, Qing Hong*. WS6 induces adult hippocampal neurogenesis in correlation to its antidepressant effect on the alleviation of depressive-like behaviors of rats. Neuroscience, 2021, 473, 119-129

12.  范炳芝#, 王一鑫#, 廉霄甜, 谢维松, 于洋, 梁建华*. 三萜类化合物抗病毒的构效关系及其作用机制研究进展. 化工学报, 2020, 71(9): 4071-4101

13.  Fan Bing-Zhi, Hiasa Hiroshi, Lv Wei, Brody Scott, Yang Zhao-Yong, Aldrich Courtney, Cushman Mark, Liang Jian-Hua*. Design, Synthesis and Structure-activity Relationships of Novel 15-Membered Macrolides: Quinolone/quinoline-containing Sidechains Tethered to the C-6 Position of Azithromycin Acylides. European Journal of Medicinal Chemistry, 2020, 193, 112222

14.  Zhang Liang, Gao Yanan, Liu Xiaofei, Guo Fang, Ma Congxuan, Liang Jianhua, Feng Xudong*, Chun Li. Mining of Sucrose Synthases from Glycyrrhiza uralensis and Their Application in the Construction of an Efficient UDP-Recycling System. Journal of Agricultural and Food Chemistry. 2019, 67(42), 11694-11702

15.  Li Xue-Meng, Lv Wei, Guo Si-Yang, Li Ya-Xin, Fan Bing-Zhi, Cushman Mark, Kong Fan-Sheng, Zhang Jun, Liang Jian-Hua*. Synthesis and Structure-bactericidal Activity Relationships of Non-ketolides: 9-Oxime Clarithromycin 11,12-Cyclic Carbonate Featured with Three- to Eight-atom-length Spacers at 3-OH. European Journal of Medicinal Chemistry, 2019, 171, 235-254

16.  Ma Cong-Xuan, Lv Wei, Li Ya-Xin, Fan Bing-Zhi, Han Xu, Kong Fan-Sheng, Tian Jing-Chao, Cushman Mark, Liang Jian-Hua*. Design, Synthesis and Structure-activity Relationships of Novel Macrolones: Hybrids of 2-Fluoro 9-Oxime Ketolides and Carbamoyl Quinolones with Highly Improved Activity against Resistant Pathogens. European Journal of Medicinal Chemistry, 2019, 169, 1-20

17.  Yang Liang, Ran Yuanyuan, Quan Zhenzhen, Wang Ran, Yang Qinghu, Jia Qiutian, Zhang Heao, Li Yanhui, Peng Yiheng, Liang JianHua, Wang Hui, Nakanishi Hiroshi, Deng Yulin*, Qing Hong*. Pterostilbene, an active component of the dragon’s blood extract, acts as an antidepressant in adult rats. Psychopharmacology, 2019, 236, 1323-1333.

18.  Liang Jian-Hua*#, Yang Liang#, Wu Si#, Liu Si-Si, Cushman Mark, Tian Jing, Li Nuo-Min, Yang Qing-Hu, Zhang He-Ao, Qiu Yun-Jie, Xiang Lin, Ma Cong-Xuan, Li Xue-Meng, Qing Hong*. Discovery of Efficient Stimulators for Adult Hippocampal Neurogenesis Based on Scaffolds in Dragon's Blood. European Journal of Medicinal Chemistry, 2017, 136, 382-392.

19.  Tian Jing-Chao, Han Xu, Lv Wei, Li Ya-Xin, Wang Hui, Fan Bing-Zhi, Cushman Mark, Liang Jian-Hua*. Design, Synthesis and Structure-bactericidal Activity Relationships of Novel 9-Oxime Ketolides and Reductive Epimers of Acylides. Bioorganic & Medicinal Chemistry Letters, 2017, 27(7): 1513-1524

20.  吴思, 庆宏, 梁建华*. 促海马区成体神经发生药物的研究进展. 药学学报 (Acta Pharmaceutica Sinica), 2016, 51(7): 1025-1031

21.  Han Xu, Lv Wei, Guo Si-Yang, Cushman Mark, Liang Jian-Hua*. Synthesis and structure-activity relationship of novel 9-oxime acylides with improved bactericidal activity. Bioorganic & Medicinal Chemistry, 2015, 23(19): 6437-6453

22.  Liang Jian-Hua*. Introduction of a nitrogen-containing sidechain appended on C-10 of cethromycin leads to reduced CYP3A4 inhibition (WO2014049356A1). Expert Opinion On Therapeutic Patents, 2015, 25(1): 119-123 (Invited Review)

23.  Liang Jian-Hua*, Han Xu. Structure-activity relationships and mechanism of action of macrolides derived from erythromycin as antibacterial agents. Current Topics in Medicinal Chemistry, 2013, 13(24):3131-3164 (Invited Review)

24.  Liang Jian-Hua*#, Lv Wei#, Li Xiao-Li, An Kun, Cushman Mark, Wang He, Xu Ying-Chun. Synthesis and antibacterial activity of 9-oxime ether non-ketolides, and novel binding mode of alkylides with bacterial rRNA. Bioorganic & Medicinal Chemistry Letters, 2013, 23(5): 1387-1393.

25.  Liang Jian-Hua*, An Kun, Lv Wei, Cushman Mark*, Wang He, Xu Ying-Chun. Synthesis, antibacterial activity and docking of 14-membered 9-O-(3-arylalkyl) oxime 11,12-cyclic carbonate ketolides. European Journal of Medicinal Chemistry, 2013, 59, 54-63.

26.  Liang Jian-Hua*, Li Xiao-Li, Wang He, An Kun, Wang Yue-Ying, Xu Yin-Chun, Yao Guo-Wei. Structure-activity relationships of novel alkylides: 3-O-arylalkyl clarithromycin derivatives with improved antibacterial activities. European Journal of Medicinal Chemistry, 2012, 49, 289-303.

27.  Cinelli Maris A., Reddy P. V. Narashimha, Lv Peng-Cheng, Liang Jian-Hua, Chen Lian, Agama Keli, Pommier Yves, Breemen Richard B. van, Cushman Mark*. Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs Indotecan (LMP400) and Indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons. Journal of Medicinal Chemistry, 2012, 55, 10844-10862.

28.  Liang Jian-Hua*, Dong Li-Jin, Wang Yue-Ying, Yao Guo-Wei, An Mao-Mao, Wang Rui. Synthesis and antibacterial activity of 2, 3-dehydro-3-O-(3-aryl-E-prop-2-enyl)-10, 11-anhydroclarithromycin derivatives. Journal of Antibiotics, 2011, 64(4): 333-337.

29.  Liang Jian-Hua*, Dong Li-Jin, Wang He, An Kun, Li Xiao-Li, Yang Li, Yao Guo-Wei, Xu Yin-Chun. Synthesis and antibacterial activities of 6-O-methylerythromycin A 9-O-(3-aryl-2-propenyl) oxime ketolide, 2,3-enol ether, and alkylide analogues. European Journal of Medicinal Chemistry, 2010, 45 (9): 3627-3635.

30.  Liang Jian-Hua*, Wang Yue-Ying, Wang He, Li Xiao-Li, An Kun, Xu Ying-Chun, Yao Guo-wei. Synthesis and antibacterial activities of a novel alkylide: 3-O-(3-aryl-2-propargyl) and 3-O-(3-aryl-2-propenyl)clarithromycin derivatives. Bioorganic & Medicinal Chemistry Letters, 2010 , 20 (9): 2880-2883.

31.  Liang Jian-Hua*, Wang Yue-Ying, Zhu Dan-Yang, Dong Li-Jing, An Mao-Mao, Wang Rui, Yao Guo-Wei. Design, synthesis and antibacterial activity of a novel alkylide: 3-O-(3-aryl-propenyl)clarithromycin derivatives. Journal of Antibiotics, 2009, 62 (11): 605-611.

32.  Liang Jian-Hua*, Yao Guo-Wei. A new crystal structure of clarithromycin. Journal of Chemical Crystallography, 2008, 38(1): 61-64.


代表性论文(理性药物设计、计算机与人工智能药物设计方向)

[1]    Zi-Qiang Feng, Jing Ding, Min-Zhen Zhu, Wei-Song Xie, Rui-Chen Liu, Si-Si Liu, Si-Meng Liu, Ming-Jia Yu*, Xin-Hong Zhu*, Jian-Hua Liang*. Discovery of a novel lead characterized by a stilbene-extended scaffold against sepsis as soluble epoxide hydrolase inhibitors. Eur. J. Med. Chem., 2024, 266:116113.

[2]    Yue Ran, Kiran Shehzadi, Jian-Hua Liang* and Ming-Jia Yu*. Rationally Designed Novel Antimicrobial Peptides Targeting Chitin Synthase for Combating Soybean Phytophthora Blight. Int. J. Mol. Sci., 2024, 25(6), 3512.

[3]    Kiran Shehzadi, Afsheen Saba, Mingjia Yu*, Jianhua Liang*. Structure-Based Drug Design of RdRp Inhibitors against SARS-CoV-2. Top. Curr. Chem., 2023, 381(5):22.

[4]    Tianji Zhang#, Mingjia Yu#, Honglian Li, Marco Maccarana, Wei Zhang, Deling Shi, Ying Kan, Xiao Zhang, Lianli Chi, Ulf Lindahl, Hongmei Li*, Jin-ping Li*, Tianwei Tan*. Interacting polymer-modification enzymes in heparan sulfate biosynthesis. Carbohydr. Polym., 2023, 299: 120191.

[5]    Kiran Shehzadi, Mingjia Yu* and Jianhua Liang*. De Novo Potent Peptide Nucleic Acid Antisense Oligomer Inhibitors Targeting SARS-CoV-2 RNA-Dependent RNA Polymerase via Structure-Guided Drug Design. Int. J. Mol. Sci., 2023, 24(24), 17473.

[6]    Binjie Li, Tianji Zhang, Hui Cao, Vito Ferro, Jinping Li*, and Mingjia Yu*. Identification of a Pentasaccharide Lead Compound with High Affinity to the SARS-CoV-2 Spike Protein via In Silico Screening. Int. J. Mol. Sci., 2023, 24, 16115.

[7]    Xiaotian Lian, Wentian Liu, Bingzhi Fan, Mingjia Yu*, and Jianhua Liang*. Design, Synthesis and Biological Evaluation of Conjugates of 3-O-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains. Molecules, 2023, 28, 3: 1327.

[8]    Mingjia Yu, Huimin Zhao, Yuhui Miao, Shi-Zhong Luo, Song Xue*. Virtual evolution of HVEM segment for checkpoint inhibitor discovery. Int. J. Mol. Sci., 2021, 21;22(12):6638.

[9]    Mingjia Yu, Tianji Zhang, Wei Zhang, Qianyun Sun, Hongmei Li*, Jin-ping Li*, Elucidating the Interactions Between Heparin/Heparan Sulfate and SARS-CoV-2-Related Proteins—An Important Strategy for Developing Novel Therapeutics for the COVID-19 Pandemic. Front. Mol. Biosci., 2021, 7:628551.

[10] Binjie Li, Tianji Zhang, Jin-ping Li, Ming-jia Yu*. Identification of Potential Antiviral Disaccharide Leading Compounds against SARS-CoV-2 through A Computer Aided Study. ChemBioChem, 2022, 23(24):e202200461.

[11] Mingjia Yu*, Tianji Zhang, Jin Ping Li, Yingxia Tan*. Elucidating the Binding Mode between Heparin and Inflammatory Cytokines by Molecular Modeling. Chemistryopen, 2021, 10(10):966-975.

[12] Ying Han, Yifan Da, Mingjia Yu, Yaping Cheng, Xin Wang, Jiale Xiong, Guoying Guo, Yan Li, Xianxing Jiang, Xiaoqing Cai*, Protein labeling approach to improve lysosomal targeting and efficacy of antibody-drug conjugates. Org. Biomol. Chem., 2020, 18(17):3229-3233.

[13] Ming-jia Yu, Shi-Lu Chen*. From Alkane to Alkene: The Inert Aliphatic C−H Bond Activation Presented by Binuclear Iron Stearoyl-CoA Desaturase with a Long di-Fe Distance of 6 Å. ACS Catal., 2019, 9: 4345-4359.

[14] Ming-jia Yu, Shi-Lu Chen*. Mechanism and inhibitor exploration for binuclear Mg ketol-acid reductoisomerase: targeting on the biosynthetic pathway of branched-chain amino acids. ChemBioChem, 2019, 21(3): 381-391.

[15] Wenya Tian, Chenghai Sun, Mei Zheng, Jeffrey Harmer, Mingjia Yu, Yanan Zhang, Haidong Peng, Dongqing Zhu, Zixin Deng, Shi-Lu Chen, Mehdi Mobli, Xinying Jia, and Xudong Qu*, Efficient Biosynthesis of Heterodimeric C3-Aryl Pyrroloindoline Alkaloids. Nat. Commun., 2018, 9: 4428(1-9).

[16] Ming-jia Yu and Shi-Lu Chen*, From NAD+ to Ni Pincer Complex: A Significant Cofactor Evolution Presented by Lactate Racemase. Chem. — Eur. J., 2017, 23(31): 7545-7557.

[17] Xianyi Mei, Xiaoli Yan, Hui Zhang, Mingjia Yu, Guangqing Shen, Linjun Zhou, Zixin Deng, Chun Lei, and Xudong Qu*, Expanding the Bioactive Chemical Space of Anthrabenzoxocinones through Engineering the Highly Promiscuous Biosynthetic Modification Steps. ACS Chem. Biol., 2017, 13(1): 200-206.

[18] Binjie Li, Huimin Zhao, Mingjia Yu*. Techniques for Detection of Clinical Used Heparins. International Journal of Analytical Chemistry. vol. 2021, Article ID 5543460, 11 pages, 2021. https://doi.org/10.1155/2021/5543460.

[19] Mingjia Yu, Zheng Dai, Xudong Qu*, Xu Gao*, Draft Genome Sequence of Marine Bacterium Streptomyces sp. Strain CNQ431, a Producer of the Cytokine Inhibitor Splenocin. Genome Announc., 2015, 3(1) e01383-14.

[20] 采用smiles算法随机批量生成肝素类似物结构坐标的方法,于明加;郭霄亮;林煌;李晋萍,授权专利号:ZL202110590305.2

[21] Liu Xingzhou, Yu Mingjia*, Liang Jianhua*. Research Progress on the Synthesis of Protoberberine Skeleton and its Anti-inflammatory Activity[J]. Chinese Journal of Organic Chemistry, 2023, doi: 10.6023/cjoc202209037.