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J-GLOBAL ID：202202267074707866   整理番号：22A0562080

2-アリール-1H-ピラゾール-S-DABOのC6構造最適化:抗HIVから抗DENV活性まで【JST・京大機械翻訳】

C6-structural optimizations of 2-aryl-1H-pyrazole-S-DABOs: From anti-HIV to anti-DENV activity

著者 (17件)： Rui Ruo-Mei (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Tang Cheng-Run (Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sc...) ,  Tang Cheng-Run (School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, Yunnan, China) ,  Zhang Chun-Tao (Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sc...) ,  Pan Wen-Kai (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Gan Kai (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Luo Rong-Hua (Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sc...) ,  Wei Zi-Qian (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Jing Fan-Shun (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Huang Si-Ming (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Yang Liu-Meng (Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sc...) ,  Li Yi-Ming (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Wang Yue-Ping (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Xiao Wei-Lie (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Zhang Hong-Bing (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China) ,  Zheng Yong-Tang (Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sc...) ,  He Yan-Ping (Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China)
資料名： Bioorganic Chemistry  (Bioorganic Chemistry)
巻： 119  ページ： Null  発行年： 2022年 
JST資料番号： E0823A  ISSN： 0045-2068  資料種別： 逐次刊行物 (A)
記事区分： 原著論文  発行国： オランダ (NLD)  言語： 英語 (EN)

抄録/ポイント： HIVとDENVは,今日,人間の生活,健康と社会経済への重大な脅威である。今まで,HIVまたはDENVに対するワクチンは成功していない。抗HIVまたはDENV薬に関する研究は,まだ大きな意義がある。本研究では,強力なNNRTIsとしてC_6-スクトルカット最適化を有する一連の新規2-アリール-1H-ピラゾール-S-DABOを開発し,その中で8つの化合物は0.05080.0966μMの範囲の低い細胞毒性とEC_50値を持ち,それらの選択性指数はSI>14153940であった。特に,2つの化合物4aと4bは,4つの血清型のDENVに良い抑制効果を持つと同定された。DENV-IIに対する化合物4aおよび4bのEC_50(それぞれ13.2μMおよび9.23μM)は,陽性対照リバビリン(EC_50=40.78μM)よりも良好であった。さらに,これらの化合物の抗HIVまたは抗DENV活性に及ぼすC-6置換基の影響も検討した。Copyright 2022 Elsevier B.V., Amsterdam. All rights reserved. Translated from English into Japanese by JST.【JST・京大機械翻訳】

シソーラス用語： *最適化 ,  ワクチン ,  細胞毒性 ,  血清型 ,  *HIV【ウイルス】 ,  *構造最適化
準シソーラス用語： 社会経済 , 【Automatic Indexing@JST】

著者キーワード (5件)： HIV-1 ,  NNRTI ,  S-DABOs DENV ,  抗ウイルス活性 ,  SAR

分類 (1件)： 酵素一般  (EB09010D)

タイトルに関連する用語 (5件)： 1H-ピラゾール ,  C6 ,  構造最適化 ,  HIV ,  活性