Art

J-GLOBAL ID：201502209493528447   Reference number：15A1184695

Design of HIV-1 Protease Inhibitors with Amino-bis-tetrahydrofuran Derivatives as P2-Ligands to Enhance Backbone-Binding Interactions: Synthesis, Biological Evaluation, and Protein-Ligand X-ray Studies

骨格鎖-結合性相互作用を強化するP2-リガンドとしてのアミノ-ビス-テトラヒドロフラン誘導体によるHIV-1プロテアーゼ阻害剤の設計:合成,生物学的評価,および蛋白質-配位子X線研究

Author (17)： GHOSH Arun K. (Purdue Univ., Indiana, USA) ,  MARTYR Cuthbert D. (Purdue Univ., Indiana, USA) ,  OSSWALD Heather L. (Purdue Univ., Indiana, USA) ,  SHERI Venkat Reddy (Purdue Univ., Indiana, USA) ,  KASSEKERT Luke A. (Purdue Univ., Indiana, USA) ,  CHEN Shujing (Purdue Univ., Indiana, USA) ,  AGNISWAMY Johnson (Georgia State Univ., Georgia, USA) ,  WANG Yuan-Fang (Georgia State Univ., Georgia, USA) ,  HAYASHI Hironori (Kumamoto Univ. Graduate School of Biomedical Sci., Kumamoto, JPN) ,  HAYASHI Hironori (National Center for Global Health and Medicine, Tokyo, JPN) ,  AOKI Manabu (Kumamoto Univ. Graduate School of Biomedical Sci., Kumamoto, JPN) ,  AOKI Manabu (National Inst. of Health, Maryland, USA) ,  AOKI Manabu (Kumamoto Health Sci. Univ., Kumamoto, JPN) ,  WEBER Irene T. (Purdue Univ., Indiana, USA) ,  MITSUYA Hiroaki (Kumamoto Univ. Graduate School of Biomedical Sci., Kumamoto, JPN) ,  MITSUYA Hiroaki (National Center for Global Health and Medicine, Tokyo, JPN) ,  MITSUYA Hiroaki (National Inst. of Health, Maryland, USA)
Material： Journal of Medicinal Chemistry  (J Med Chem)
Volume： 58  Issue： 17  Page： 6994-7006  Publication year： Sep. 10, 2015 
JST Material Number： D0102A  ISSN： 0022-2623  CODEN： JMCMAR  Document type： Article
Article type： 原著論文  Country of issue： United States (USA)  Language： ENGLISH (EN)

Thesaurus term： *cyclic ether ,  *oxygen heterocyclic compound ,  proteinase inhibitor ,  stereoselectivity ,  *antiviral action ,  multiple drug resistance ,  X-ray diffraction ,  chemical synthesis ,  molecular structure ,  *structure-activity relationship
Semi thesaurus term： HIV-1 protease inhibitors ,  Drug Resistance, Multiple, Viral ,  diastereofacial selectivity ,  *tetrahydrofuran derivative ,  *antiviral activity ,  high-resolution X-ray diffraction

JST classification (3)： Condensed derivatives of furan  (CF07073M) ,  Basic research of antiviral drugs  (GW17040O) ,  Structure-activity relationship of drugs  (GV01050B)

Substance index (15)： (Z)-2,2-Dimethyl-1,3-dioxolane-4β-acrylic acid ethyl ester ,  (3R,3aS,4R,6aR)-4-Azidohexahydrofuro[2,3-b]furan-3-ol ,  ((3R,3aS,4R,6aR)-4-Azidohexahydrofuro[2,3-b]furan-3-yl)benzyl ether ,  ((3R,3aS,4R,6aR)-4-Benzyloxyhexahydrofuro[2,3-b]furan-3-yl)carbamic acid methyl ester ,  N-Boc-((3R,3aS,4R,6aR)-4-Benzyloxyhexahydrofuro[2,3-b]furan-3-yl)isopropylamine ,  N-Boc-((3R,3aS,4R,6aR)-4-Benzyloxyhexahydrofuro[2,3-b]furan-3-yl)methylamine ,  N-Boc-((3R,3aS,4R,6aR)-4-Benzyloxyhexahydrofuro[2,3-b]furan-3-yl)amine ,  N-Boc-((3R,3aS,4R,6aR)-4-Benzyloxyhexahydrofuro[2,3-b]furan-3-yl)ethylamine ,  (3R,3aS,4R,6aR)-4-(N-Boc-Amino)hexahydrofuro[2,3-b]furan-3-ol ,  ((3R,3aS,4R,6aR)-4-Hydroxyhexahydrofuro[2,3-b]furan-3-yl)carbamic acid methyl ester ,  (3R,3aS,4R,6aR)-4-(N-Boc-Methylamino)hexahydrofuro[2,3-b]furan-3-ol ,  Carbonic acid ((3R,3aS,4R,6aR)-4-azidohexahydrofuro[2,3-b]furan-3-yl)(4-nitrophenyl) ester ,  (2R,3S)-1-((4-Methoxyphenylsulfonyl)isobutylamino)-3-amino-4-phenylbutane-2-ol ,  ((2S,3R)-1-Phenyl-3-hydroxy-3-((4-methoxyphenylsulfonyl)isobutylamino)butane-2-yl)carbamic acid ((3R,3aS,4R,6aR)-4-azidohexahydrofuro[2,3-b]furan-3-yl) ester ,  ((2S,3R)-1-Phenyl-3-hydroxy-3-((4-methoxyphenylsulfonyl)isobutylamino)butane-2-yl)carbamic acid ((3R,3aS,4R,6aR)-4-aminohexahydrofuro[2,3-b]furan-3-yl) ester

Terms in the title (14)： 骨格 ,  結合性 ,  相互作用 ,  強化 ,  リガンド ,  ビス ,  テトラヒドロフラン誘導体 ,  HIV-1プロテアーゼ阻害剤 ,  設計 ,  生物学的評価 ,  蛋白質 ,  配位子 ,  X線 ,  研究