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| 1 | Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives显示文摘A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities.The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity.Notably,compound 8f showed the highest SI value(17.1)to Cox B3 virus.Compound 14f showed both potent inhibitory activity against influenza A(IC_(50)=7.53μmol/L)and the highest SI value(12.1).SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities.Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses. | Situ Xue Linlin Ma Rongmei Gao Yuhuan Li Zhuorong Li | 2014 | Acta Pharmaceutica Sinica B2014，4，4： | 3 |
| 2 | Synthesis of novel substituted N-aryl benzamides as hA3G stabilizers and their inhibitory activities against hepatitis C virus replication显示文摘A series of novel amino-substituted N-aryl benzamide analogs were synthesized and evaluated for their ability to inhibit hepatitis C virus(HCV)replication in acutely infected Huh7.5 cells.Most of the substituted N-aryl benzamide compounds showed convincing anti-HCV activities.Compounds 1f,1g and 4c exhibited potent anti-replicative activity at low micromolar levels(IC_(50)=1.0–2.0μM)with selective indices(SI)greater than 40.Mechanistic analysis indicated that the active compounds increased intracellular hA3G protein levels and inhibited HCV replication in a dose-dependent manner.The results demonstrate that this series of substituted Naryl benzamide compounds warrant further investigation as inhibitors of HCV replication. | Yanping Li Zonggen Peng Lanhu Hao Zhouyi Wu Yanping Zhu Laixing Hu Jiandong Jiang Zhuorong Li | 2013 | Acta Pharmaceutica Sinica B2013，3，5： | 2 |
| 3 | Polymyxin resistance caused by large-scale genomic inversion due to IS26 intramolecular translocation in Klebsiella pneumoniae显示文摘Polymyxin B and polymyxin E(colistin)are presently considered the last line of defense against human infections caused by multidrug-resistant Gram-negative organisms such as carbapenemase-producer Enterobacterales,Acinetobacter baumannii,and Klebsiella pneumoniae.Yet resistance to this last-line drugs is a major public health threat and is rapidly increasing.Polymyxin S2(S2)is a polymyxin B analogue previously synthesized in our institute with obviously high antibacterial activity and lower toxicity than polymyxin B and colistin.To predict the possible resistant mechanism of S2for wide clinical application,we experimentally induced bacterial resistant mutants and studied the preliminary resistance mechanisms.Mut-S,a resistant mutant of K.pneumoniae ATCC BAA-2146(Kpn2146)induced by S2,was analyzed by whole genome sequencing,transcriptomics,mass spectrometry and complementation experiment.Surprisingly,large-scale genomic inversion(LSGI)of approximately 1.1 Mbp in the chromosome caused by IS26mediated intramolecular transposition was found in Mut-S,which led to mgrB truncation,lipid A modification and hence S2resistance.The resistance can be complemented by plasmid carrying intact mgrB.The same mechanism was also found in polymyxin B and colistin induced drug-resistant mutants of Kpn2146(Mut-B and Mut-E,respectively).This is the first report of polymyxin resistance caused by IS26 intramolecular transposition mediated mgrB truncation in chromosome in K.pneumoniae.The findings broaden our scope of knowledge for polymyxin resistance and enriched our understanding of how bacteria can manage to survive in the presence of antibiotics. | Haibin Li Lang Sun Han Qiao Zongti Sun Penghe Wang Chunyang Xie Xinxin Hu Tongying Nie Xinyi Yang Guoqing Li Youwen Zhang Xiukun Wang Zhuorong Li Jiandong Jiang Congran Li Xuefu You | 2023 | Acta Pharmaceutica Sinica B2023，13，9： | 1 |
| 4 | Synthesis and antiviral activities of a novel class of thioflavone and flavonoid analogues显示文摘A novel class of thioflavone and flavonoid derivatives has been prepared and their antiviral activities against enterovirus 71(EV71)and the coxsackievirus B3(CVB3)and B6(CVB6)were evaluated.Compounds 7d and 9b showed potent antiviral activities against EV71 with ICso values of 8.27 and 5.48μM,respectively.Compound 7f,which has been synthesized for the first time in this work,showed the highest level of inhibitory activity against both CVB3 and CVB6 with an ICso value of 0.62 and 0.87μM.Compounds 4b,7a,9c and 9e also showed strong inhibitory activities against both the CVB3 and CV B6 at low concentrations(IC_(50)=1.42-7.15μM),whereas compounds 4d,7c,7e and 7g showed strong activity against CVB6(IC_(50)=2.91-3.77μM)together with low levels of activity against CVB3.Compound 7d exhibited stronger inhibitory activity against CVB3(IC_(50)=6.44μM)thaln CVB6(IC_(50)>8.29μM).The thioflavone derivatives 7a,7c,7d,7e,7f and 7g,represent a new class of lead compounds for the development of novel antiviral agents. | Dajun Zhang Xingyue Ji Rongmei Gao Huiqiang Wang Shuai Meng Zhaojin Zhong Yuhuan Lin Jiandong Jiang Zhuorong Li | 2012 | Acta Pharmaceutica Sinica B2012，2，6： | 0 |
| 5 | An Error-Correcting Code-Based Robust Watermarking Scheme for Stereolithographic Files显示文摘Stereolithographic(STL)files have been extensively used in rapid prototyping industries as well as many other fields as watermarking algorithms to secure intellectual property and protect three-dimensional models from theft.However,to the best of our knowledge,few studies have looked at how watermarking can resist attacks that involve vertex-reordering.Here,we present a lossless and robust watermarking scheme for STL files to protect against vertexreordering attacks.Specifically,we designed a novel error-correcting code(ECC)that can correct the error of any one-bit in a bitstream by inserting several check digits.In addition,ECC is designed to make use of redundant information according to the characteristics of STL files,which introduces further robustness for defense against attacks.No modifications are made to the geometric information of the three-dimensional model,which respects the requirements of a highprecision model.The experimental results show that the proposed watermarking scheme can survive numerous kinds of attack,including rotation,scaling and translation(RST),facet reordering,and vertex-reordering attacks. | Zhuorong Li Huawei Tian Yanhui Xiao Yunqi Tang Anhong Wang | 2021 | Computer Systems Science & Engineering2021，37，5： | 0 |
| 6 | Molecular modeling of human APOBEC3G to predict the binding modes of the inhibitor compounds IMB26 and IMB35显示文摘APOBEC3G(A3G)is a host cytidine deaminase that incorporates into HIV-1 virions and efficiently inhibits viral replication.The virally encoded protein Vif binds to A3G and induces its degradation,thereby counteracting the antiviral activity of A3G.Vif-mediated A3G degradation clearly represents a potential target for anti-HIV drug development.Currently,there is an urgent need for understanding the three dimensional structure of full-length A3G.In this work,we use a homology modeling approach to propose a structure for A3G based on the crystal structure of APOBEC2(APO2)and the catalytic domain structure of A3G.Two compounds,IMB26 and IMB35,which have been shown to bind to A3G and block degradation by Vif,were docked into the A3G model and the binding modes were generated for further analysis.The results may be used to design or optimize molecules targeting Vif–A3G interaction,and lead to the development of novel anti-HIV drugs. | Zhixin Zhang Congjie Zhai Zeyun Mi Jiwei Ding Yongxin Zhang Xing Shi Xiaoyu Li Liyan Yu Zhuorong Li Jiandong Jiang Jinming Zhou Shan Cen | 2013 | Acta Pharmaceutica Sinica B2013，3，4： | 0 |
| 7 | An Efficient Sleep Spindle Detection Algorithm Based on MP and LSBoost显示文摘Sleep spindles are an electroencephalogram(EEG)biomarker of non-rapid eye movement(NREM)sleep and have important implications for clinical diagnosis and prognosis.However,it is challenging to accurately detect sleep spindles due to the complexity of the human brain and the uncertainty of neural mechanisms.To improve the reliability and objectivity of sleep spindle detection and to compensate for the limitations of manual annotation,this study proposes a new automatic detection algorithm based on Matching Pursuit(MP)and Least Squares Boosting(LSBoost),where the automatic sleep spindle detection algorithm can help reduce the visual annotation workload of sleep clinicians.Specifically,MP is a time-frequency analysis method suitable for extracting spindle wave characteristics,which can accurately locate spindle waves on a time-frequency plane.LSBoost is an ensemble learning classification method to deal with unbalanced data.Initially,theMP method is used to search for EEG segments that are possible spindle waves from the filtered raw EEG data.Then,the designed feature segments are thrown into the LSBoost classifier to further identify the real spindles from all candidates and output the final results.The proposed method is verified on the common public dataset DREAMS.The experiment results showthat the sensitivity and F1-scores based on the sample-based assessments achieve 68.2% and 55.4%,respectively.Furthermore,the Recall and F1-score based on the event assessments are 83.8% and 70.8%,respectively.These results show that the proposed algorithm is robust to the subject changes in the DREAMS dataset.In addition,it improves the quality of sleep spindle detection,which is expected to assist the manual marking of experts. | Fei Wang Li Li Yinxing Wan Zhuorong Li Lixian Luo Bangshun Hu Jiahui Pan Zhenfu Wen Haiyun Huang | 2023 | Computers, Materials & Continua2023，76，8： | 0 |
| 8 | Multimodal Biometric Fusion Algorithm Based on Ranking Partition Collision Theory显示文摘Score-based multimodal biometric fusion has been shown to be successful in addressing the problem of unimodal techniques’vulnerability to attack and poor performance in low-quality data.However,difficulties still exist in how to unify the meaning of heterogeneous scores more effectively.Aside from the matching scores themselves,the importance of the ranking information they include has been undervalued in previous studies.This study concentrates on matching scores and their ranking information and suggests the ranking partition collision(RPC)theory from the standpoint of the worth of scores.To meet both forensic and judicial needs,this paper proposes a method that employs a neural network to fuse biometrics at the score level.In addition,this paper constructs a virtual homologous dataset and conducts experiments on it.Experimental results demonstrate that the proposed method achieves an accuracy of 100%in both mAP and Rank1.To show the efficiency of the proposed method in practical applications,this work carries out more experiments utilizing real-world data.The results show that the proposed approach maintains a Rank1 accuracy of 99.2%on the million-scale database.It offers a novel approach to fusion at the score level. | Zhuorong Li Yunqi Tang | 2023 | Machine Intelligence Research2023，20，6： | 0 |
| 9 | THE COMPARISON THEOREMS OF WEIGHTED ADDITIVE SCHWARZ METHODS显示文摘Consider the linear systemAx=b,(1)where A∈Rn×n is nonsingular.The additive Schwarz method was introduced in the last century.Recently,themethod has been used for solving general algebraic system of linear equations (1) in paral-lel computer (see [1]).This iterative method can be considered as a general multisplit-ting,in which the corresponding iterates xn,l,l=1,2,…,k,are given | Chen Zhuorong Li Wen(Dept.of Math.,South China Normal University,Guangzhou 510631,PRC) | 2000 | Numerical Mathematics A Journal of Chinese Universities(English Series)2000，9，S1： | 0 |
| 10 | IMB-0523 Inhibits Enterovirus 71 Replication by Activating Signal Transducer and Activator of Transcription 3 Signaling to Upregulate Interferon-Stimulated Genes Expression显示文摘Background Hand,foot,and mouth disease caused by enterovirus 71(EV71)infection is prevalent in the Asia-Pacific region in recent years.Currently,no drug is available for the prevention and treatment of EV71 infection.IMB-0523,a N-phenylbenzamide derivative,inhibits hepatitis B virus replication by upregulating the expression of APOBEC3G.In the present study,the effect of IMB-0523 on EV71 replication and related mechanism were investigated.Methods The cytotoxicity of IMB-0523 was determined by cell counting kit.Quantitative real-time polymerase chain reaction and Western blot assay were used to detect the effect of IMB-0523 on EV71 replication and related mechanism.Cytopathic effect assay was used to investigate the effect of IMB-0523 on different EV71 strains,coxsackievirus A16,and coxsackieviruses of group B.Results The results showed that IMB-0523 could dose-dependently inhibit EV71 replication.Preliminary mechanism studies showed that IMB-0523 could activate STAT3 signaling to upregulate the expression of interferon-stimulated genes to play an antiviral role.In addition,IMB-0523 inhibited the replication of different EV71 strains,coxsackievirus A16,and coxsackieviruses of group B.Conclusions IMB-0523 inhibits EV71 replication by activating the STAT3 signaling pathway to upregulate interferon-stimulated gene expression.IMB-0523 has broad-spectrum antiviral potential and may be used as a lead compound for the development of broad spectrum antiviral drugs. | Huiqiang Wang Miao Ge Yanping Li Yuhuan Li Zhuorong Li | 2023 | Infectious Diseases & Immunity2023，3，1： | 0 |
| 11 | Synthesis and antiviral activity of a series of novel N-phenylbenzamide and N-phenylacetophenone compounds as anti-HCV and anti-EV71 agents显示文摘A series of novel N-phenylbenzamide and N-phenylacetophenone compounds were synthesized and evaluated for their antiviral activity against HCV and EV71(strain SZ-98).The biological results showed that three compounds(23,25 and 41) exhibited considerable anti-HCV activity(IC50? 0.57–7.12 μmol/L) and several compounds(23,28,29,30,31 and 42) displayed potent activity against EV71 with the IC50 values lower than 5.00 μmol/L.The potency of compound 23(IC50? 0.57 μmol/L) was superior to that of reported compounds IMB-1f(IC50? 1.90 μmol/L) and IMB-1g(IC50? 1.00 μmol/L) as anti-HCV agents,and compound29 possessed the highest anti-EV71 activity,comparable to the comparator drug pirodavir.The efficacy in vivo and antiviral mechanism of these compounds warrant further investigations. | Zhi Jiang Huiqiang Wang Yanping Li Zonggen Peng Yuhuan Li Zhuorong Li | 2015 | Acta Pharmaceutica Sinica B2015，5，3： | 0 |
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