文献

J-GLOBAL ID：202202234071203664   整理番号：22A0324856

新しいHBVカプシド集合モジュレーターとしての(6S)-シクロプロピル-6,7-ジヒドロピラゾロ[1,5-a]ピラジン-5(4H)-カルボキサミンの同定【JST・京大機械翻訳】

Identification of (6S)-cyclopropyl-6,7-dihydropyrazolo[1,5-a]pyrazine-5(4H)-carboxamines as new HBV capsid assembly modulators

著者 (17件)： Lv Kai (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Wu Shuo (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Tao Zeyu (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Wang Aoyu (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Xu Shijie (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Yang Lu (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Gao Qiang (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Wang Apeng (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Qin Xiaoyu (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Jiang Bin (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Jiang Bin (Department of Pharmaceutical Chemistry, School of Pharmacy, Hebei Medical University, Shijiazhuang, 050017, China) ,  Wu Wenhao (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Wu Wenhao (Department of Pharmaceutical Chemistry, School of Pharmacy, Hebei Medical University, Shijiazhuang, 050017, China) ,  Jia Xuedong (The First Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China) ,  Li Yuhuan (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Jiang Jiandong (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China) ,  Liu Mingliang (CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China)
資料名： European Journal of Medicinal Chemistry  (European Journal of Medicinal Chemistry)
巻： 228  ページ： Null  発行年： 2022年 
JST資料番号： E0845A  ISSN： 0223-5234  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： GYH2-18は,Roche INCによって発見された6,7-ジヒドロピラゾロ[1,5-a]ピラジン-5(4H)-カルボキサミン(DPPC)骨格を有するII型HBVCAMである。一連のGYH2-18誘導体を設計し,合成し,それらの抗HBV活性を評価した。2つの化合物2fおよび3kは,優れた抗HBV活性,低い細胞毒性および受け入れられた経口PKプロファイルを示した。2f及び3kのキラル分離を成功裏に行い,(6S)-シクロプロピルDPPC異性体2f-1,2f-3,3k-1及び3k-3を対応する(6R)-オンよりも遥かに活性であると同定した。予備的構造活性相関,粒子ゲルアッセイおよび分子モデリング研究も議論し,新しい(6S)-シクロプロピルDPPC類似体のさらなる合理的設計を導くための有用な適応を提供した。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： *変調器 ,  構造活性相関 ,  細胞毒性 ,  化合物 ,  活性 ,  異性体 ,  類似物質 ,  *カプシド
準シソーラス用語： キラル分離 ,  分子モデリング , 【Automatic Indexing@JST】

著者キーワード (4件)： カプシドアセンブリ変調器 ,  HBV感染 ,  (6S)-シクロプロピル-67-ジヒドロピラゾロ[15-a]ピラジン-5(4H)-カルボキサミン類 ,  構造活性相関

分類 (1件)： 抗ウイルス薬の基礎研究  (GW17040O)

タイトルに関連する用語 (6件)： HBV ,  カプシド ,  集合 ,  モジュレーター ,  ピラジン ,  同定