共查询到20条相似文献,搜索用时 125 毫秒
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Synthesis,Biological Evaluation and Molecular Modeling Studies of New 2,3‐Diheteroaryl Thiazolidin‐4‐Ones as NNRTIs
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Utsab Debnath Saroj Verma Pankaj Singh Kavita Rawat Satish K. Gupta Raj K. Tripathi Hefazat H. Siddiqui Seturam B. Katti Yenamandra S. Prabhakar 《Chemical biology & drug design》2015,86(5):1285-1291
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Design,synthesis, and biological evaluation of novel 5‐Alkyl‐6‐Adamantylmethylpyrimidin‐4(3H)‐ones as HIV‐1 non‐nucleoside reverse‐transcriptase inhibitors
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Wenxin Li Boshi Huang Dongwei Kang Erik De Clercq Dirk Daelemans Christophe Pannecouque Peng Zhan Xinyong Liu 《Chemical biology & drug design》2016,88(3):380-385
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Design,Synthesis, and Biological Evaluation of Novel 4‐Aminopiperidinyl‐linked 3,5‐Disubstituted‐1,2,6‐thiadiazine‐1,1‐dione Derivatives as HIV‐1 NNRTIs
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Tao Liu Boshi Huang Ye Tian Xin Liang Hong Liu Huiqing Liu Peng Zhan Erik De Clercq Christophe Pannecouque Xinyong Liu 《Chemical biology & drug design》2015,86(1):107-113
Based on the hybridization of the privileged fragments in DABO and DAPY‐typed HIV‐1 NNRTIs, a novel series of 4‐aminopiperidinyl‐linked 3,5‐disubstituted‐1,2,6‐thiadiazine‐1,1‐dione derivatives were designed, synthesized, and evaluated for their in vitro anti‐HIV activities in MT‐4 cells. Most of the target compounds showed weak inhibitory activity against WT HIV‐1. In order to confirm the mode of action of the target compounds, representative compounds Ba8 and Bb8 were selected to perform the HIV‐1 RT inhibitory assay. In this assay, Ba8 and Bb8 displayed good activity with IC50 values of 3.15 and 1.52 μm , respectively. Additionally, preliminary structure–activity relationships (SARs) analysis and molecular docking studies of newly synthesized compounds are also discussed. 相似文献
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Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5‐b]pyridin‐2‐ylthioacetanilides as Potent HIV NNRTIs Via a Structure‐based Bioisosterism Approach
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Xiao Li Boshi Huang Zhongxia Zhou Ping Gao Christophe Pannecouque Dirk Daelemans Erik De Clercq Peng Zhan Xinyong Liu 《Chemical biology & drug design》2016,88(2):241-253
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Junwon Kim Doohyun Lee Changmin Park Wonyoung So Mina Jo Taedong Ok Jeongjin Kwon Sunju Kong Suyeon Jo Youngmi Kim Jihyun Choi HyoungCheul Kim Yoonae Ko Inhee Choi Youngsam Park Jaewan Yoon MoonKyeong Ju Junghwan Kim Sung-Jun Han Tae-Hee Kim Jonathan Cechetto Jiyoun Nam Peter Sommer Michel Liuzzi Jinhwa Lee Zaesung No 《ACS medicinal chemistry letters》2012,3(8):678-682
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Wenlin Huang Tao Zuo Xiao Luo Hongwei Jin Zhenming Liu Zhenjun Yang Xianghui Yu Liangren Zhang Lihe Zhang 《Chemical biology & drug design》2013,81(6):730-741
Compound 1 (VEC‐5) was identified as a potent small‐molecular HIV‐1 viron infectivity factor inhibitor that targets the viron infectivity factor–ElonginC interaction. A structure–activity relationship study was carried out to develop compounds with improved efficacy against HIV‐1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that five compounds exhibited promising anti‐HIV‐1 activity, and the most active compound 2g had an IC50 value of 11.0 μm . These results provide new information to develop highly potent small‐molecule HIV‐1 viron infectivity factor inhibitors. 相似文献
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