NNRTIS

作品数：27被引量：25H指数：4
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相关领域：医药卫生更多>>
相关作者：刘新泳展鹏何严萍黄琴张仁芳更多>>
相关机构：山东大学云南大学军事医学科学院中国医学科学院北京协和医学院更多>>
相关期刊：《国际病毒学杂志》《药学学报》《科技创新导报》《中国药物化学杂志》更多>>
相关基金：国家自然科学基金中国博士后科学基金国家科技重大专项中央级公益性科研院所基本科研业务费专项更多>>
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Design and optimization of piperidinesubstituted thiophene[3,2-d]pyrimidine-based HIV-1 NNRTIs with improved drug resistance and pharmacokinetic profiles
《Acta Pharmaceutica Sinica B》2024年第7期3110-3124,共15页Yanying Sun Zhenzhen Zhou Zhongling Shi Fabao Zhao Minghui Xie Zongji Zhuo Erik De Clercq Christophe Pannecouqueb Dongwei Kang Peng Zhan Xinyong Liu 
financial support from the National Natural Science Foundation of China(NSFC Nos.81973181,82273773);Shandong Provincial Natural Science Foundation(ZR2020YQ61,ZR2020JQ31,China);Qilu Young Scholars Program of Shandong University and Taishan Scholar Program at Shandong Province.
HIV-1 reverse transcriptase(RT)has received great attention as an attractive therapeutic target for acquired immune deficiency syndrome(AIDS),but the inevitable drug resistance and side effects have always been major ...
关键词：HIV-1 NNRTIS NNIBP Structural alert Anti-HIV-1 drug candidate 
Design,synthesis,and biological evaluation of benzo[4,5]thieno[2,3-d]pyrimidine derivatives as novel HIV-1 NNRTIs
《Chinese Chemical Letters》2024年第6期344-348,共5页Bairu Meng Zongji Zhuo Han Yu Sining Tao Zixuan Chen Erik De Clercq Christophe Pannecouque Dongwei Kang Peng Zhan Xinyong Liu 
financial support from the National Natural Science Foundation of China(NSFC,Nos.81973181,82273773);Shandong Provincial Natural Science Foundation(Nos.ZR2020YQ61,ZR2020JQ31);Qilu Young Scholars Program of Shandong University and Taishan Scholar Program at Shandong Province。
Inspired by our previous studies to discover novel human immunodeficiency virus-1(HIV-1)nonnucleoside reverse transcriptase inhibitors(NNRTIs)by targeting the tolerant region II of the NNRTIs binding pocket(NNIBP),a s...
关键词：HIV-1 NNRTIS DAPYs Tolerant regionⅡ Drug design 
Structure-based design of novel heterocyclesubstituted ATDP analogs as non-nucleoside reverse transcriptase inhibitors with improved selectivity and solubility
《Acta Pharmaceutica Sinica B》2023年第12期4906-4917,共12页Li-Min Zhao Christophe Pannecouque Erik De Clerc Shuai Wang Fen-Er Chen 
financially supported by National Natural Science Foundation of China(No.22077018).
Following on our recently developed biphenyl-ATDP non-nucleoside reverse transcriptase inhibitor ZLM-66(SI=2019.80,S=1.9μg/mL),a series of novel heterocycle-substituted ATDP derivatives with significantly improved se...
关键词：HIV-1 RT NNRTIS ATDP PYRIDONE 
Discovery of novel sulfonamide substituted indolylarylsulfones as potent HIV-1 inhibitors with better safety profiles被引量：2
《Acta Pharmaceutica Sinica B》2023年第6期2747-2764,共18页Shenghua Gao Letian Song Yusen Cheng Fabao Zhao Dongwei Kang Shu Song Mianling Yang Bing Ye Wei Zhao Yajie Tang Erik De Clercq Christophe Pannecouque Peng Zhan Xinyong Liu 
financial support from Natural Science Foundation of China (81974507);Guangdong Basic and Applied Basic Research Foundation (2021A1515110740, China);China Postdoctoral Science Foundation (2021M702003);Shandong Province Natural Science Foundation for Youths (ZR2022QH036, China);the Foundation for Innovative Research Groups of State Key Laboratory of Microbial Technology (WZCX2021-03, China);Foreign cultural and educational experts Project (GXL20200015001, China);Science Foundation for Outstanding Young Scholars of Shandong Province (ZR2020JQ31, China);the Shandong Provincial Key research and development project (2019JZZY021011, China)。
Indolylarylsulfones(IASs) are classical HIV-1 non-nucleoside reverse transcriptase inhibitors(NNRTIs) with a unique scaffold and possess potent antiviral activity.To address the high cytotoxicity and improve safety pr...
关键词：HIV-1 NNRTIS Indolylarylsulfone SULFONAMIDE CYTOTOXICITY 
Linker optimization of HEPT derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors: From S=O to CHOR
《Chinese Chemical Letters》2023年第4期188-192,共5页Qingqing Hao Xu Ling Christophe Pannecouque Erik De Clercq Fener Chen 
financially supported by National Natural Science Foundation of China (No. 22077018);National Key R&D Program of China (No. 2017YFA0506000)。
A novel series of CHOR-HEPT non-nucleoside HIV-1 reverse transcriptase inhibitors were developed by means of structure-based design strategy based on compound 6 reported previously by our group. Most of these compound...
关键词：HIV NNRTIS HEPTs RT OPTIMIZATION 
Boronic acid-containing diarylpyrimidine derivatives as novel HIV-1NNRTIs: Design, synthesis and biological evaluation被引量：2
《Chinese Chemical Letters》2021年第12期4053-4057,共5页Da Feng Fenju Wei Yanying Sun Prem Prakash Sharma Tao Zhang Hao Lin Brijesh Rathi Erik De Clercq Christophe Pannecouque Dongwei Kang Peng Zhan Xinyong Liu 
financial support from the National Natural Science Foundation of China (Nos. 81973181, 81903453);Shandong Provincial Natural Science Foundation (No. ZR2019BH011);Natural Science Foundation of Jiangsu Province (No. BK2019041035);China Postdoctoral Science Foundation (Nos. 2019T120596, 2018M640641);Science Foundation for Outstanding Young Scholars of Shandong Province (No. ZR2020JQ31);Science Foundation for Excellent Young Scholars of Shandong Province (No. ZR2020YQ61);National Science and Technology Major Projects for "Major New Drugs Innovation and Development" (2019ZX09301126);Shandong Provincial Key Research and Development Project (Nos. 2017CXGC1401, 2019JZZY021011);Foreign cultural and educational experts Project (No. GXL20200015001);the Taishan Scholar Program at Shandong Province and KU Leuven (No. GOA 10/014)。
Drug resistance remains to be a serious problem with type Ⅰ human immunodeficiency virus(HIV-1) nonnucleoside reverse transcriptase inhibitors(NNRTIs). A series of novel boronic acid-containing diarylpyrimidine(DAPY)...
关键词：HIV-1 NNRTIS NNIBP DAPY Boronic acid Molecular dynamics simulation 
Structure-based linker optimization of 6-(2-cyclohexyl-1-alkyl)-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors被引量：1
《Chinese Chemical Letters》2021年第3期1020-1024,共5页Daxiong Li Chunsheng Zhang Wei Ding Siming Huang Le Yu Nan Lu Wenkai Pan Yiming Li Erik De Clercq Christophe Pannecouque Hongbing Zhang Yueping Wang Yanping He Fener Chen 
financial support from the National Natural Science Foundation of China(Nos.21967020,U1702286,21362017,21262044);Program for Changjiang Scholars and Innovative Research Team in University(No.IRT17R94,China);Fund of Academician Working Station of Yunnan Province(No.2018IC057)。
In continuation of our efforts toward the discovery of potent HIV-1 NNRTIs with diverse structures,a series of novel S-DACO analogues of 6-(2-cyclohexyl-1-allkyl)-2-(2-oxo-2-phenyl-ethylsulfanyl)pyrimidin-4(3 H)-ones ...
关键词：NNRTIS S-DABOs S-DACOs Anti HIV-1 activity SAR 
新型稠环嘧啶类HIV-1 NNRTIs的设计、合成、抗病毒活性与初步成药性研究被引量：1
《合成化学》2020年第7期I0003-I0003,共1页古双喜 
艾滋病(AIDS)是由人类免疫缺陷病毒(HIV)感染引起的全球重大流行性传染病。据世界卫生组织(WHO)的数据报道,截至2018年底,因感染艾滋病毒而死亡的人数达到了3200万,全球现存约有3790万艾滋病毒感染者,其中2018年新增感染人数约170万人,7...
关键词：药物协同作用 感染人数 NNRTIS 非核苷类逆转录酶抑制剂 抗病毒活性 流行性传染病 耐药株 逆转录酶 
Development of non-nucleoside reverse transcriptase inhibitors(NNRTIs):our past twenty years被引量：4
《Acta Pharmaceutica Sinica B》2020年第6期961-978,共18页Chunlin Zhuang Christophe Pannecouque Erik De Clercq Fener Chen 
funded by grants from the National Natural Science Foundation of China(81872791 and 21372050);the Young Elite Scientists Sponsorship Program by the China Association forScience and Technology(2017QNRC061);National Key R&D Program of China(2017YFA0506000);the Key Research and Development Program of Ningxia(2019BFG02017 and 2018BFH02001,China)
Human immunodeficiency virus(HIV)is the primary infectious agent of acquired immunodeficiency syndrome(AIDS),and non-nucleoside reverse transcriptase inhibitors(NNRTIs)are the cornerstone of HIV treatment.In the last ...
关键词：HIV-1 NNRTIS HENTs S-DABOs DATAs DAPYs Structure-based optimization Fragment-based drug design Molecular hybridization BIOISOSTERISM 
Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidinesubstituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs被引量：5
《Acta Pharmaceutica Sinica B》2020年第5期878-894,952,共18页Dongwei Kang Da Feng Tiziana Ginex Jinmi Zou Fenju Wei Tong Zhao Boshi Huang Yanying Sun Samuel Desta Erik DeClercq Christophe Pannecouque Peng Zhan Xinyong Liu 
financial support from the Key Project of NSFC for International Cooperation(No.81420108027,China);the National Natural Science Foundation of China(NSFC Nos.81273354,81573347,81903453);Young Scholars Program of Shandong University(YSPSDU No.2016WLJH32,China);Shandong Provincial Natural Science Foundation(ZR2019BH011,China);China Postdoctoral Science Foundation(2018M640641,2019T120596);Key research and development project of Shandong Province(No.2017CXGC1401,China);KU Leuven(GOA 10/014,Belgium);the Spanish Government(MINECO Project SAF2017-881074-R,AEI/FEDER,UE);Generalitat de Catalunya(2017SGR1746,Spain)for the financial support
In this report,a series of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives were designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket(NNI...
关键词：HIV-1 NNRTIS NNIBP Thiophene[3 2-d]pyrimidine Hydrophobic channel 
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