• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 2: Variation of the 2- and 6-pyridazinone substituents.

作者信息

Zhou Yuefen, Li Lian-Sheng, Dragovich Peter S, Murphy Douglas E, Tran Chinh V, Ruebsam Frank, Webber Stephen E, Shah Amit M, Tsan Mei, Averill April, Showalter Richard E, Patel Rupal, Han Qing, Zhao Qiang, Hermann Thomas, Kissinger Charles R, Lebrun Laurie, Sergeeva Maria V

机构信息

Anadys Pharmaceuticals, Inc., 3115 Merryfield Row, San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1419-24. doi: 10.1016/j.bmcl.2008.01.005. Epub 2008 Jan 8.

DOI:10.1016/j.bmcl.2008.01.005
PMID:18226901
Abstract

5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as inhibitors of genotype 1 HCV NS5B polymerase. The structure-activity relationship (SAR) associated with variation of the pyridazinone 2- and 6-substituents is discussed. The synthesis and metabolic stability of this new class of compounds are also described.

摘要

相似文献

1
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 2: Variation of the 2- and 6-pyridazinone substituents.
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1419-24. doi: 10.1016/j.bmcl.2008.01.005. Epub 2008 Jan 8.
2
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.源自4-(1',1'-二氧代-1',4'-二氢-1'λ6-苯并[1',2',4']噻二嗪-3'-基)-5-羟基-2H-哒嗪-3-酮的新型丙型肝炎病毒NS5B聚合酶抑制剂。第1部分:苯并噻二嗪7'-位取代基的探索。
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1413-8. doi: 10.1016/j.bmcl.2008.01.007. Epub 2008 Jan 8.
3
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 5: Exploration of pyridazinones containing 6-amino-substituents.源自4-(1',1'-二氧代-1',4'-二氢-1'λ(6)-苯并[1',2',4']噻二嗪-3'-基)-5-羟基-2H-哒嗪-3-酮的新型丙型肝炎病毒NS5B聚合酶抑制剂。第5部分:含6-氨基取代基哒嗪酮的探索。
Bioorg Med Chem Lett. 2008 Oct 15;18(20):5635-9. doi: 10.1016/j.bmcl.2008.08.094. Epub 2008 Aug 29.
4
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 3: Further optimization of the 2-, 6-, and 7'-substituents and initial pharmacokinetic assessments.源自4-(1',1'-二氧代-1',4'-二氢-1'λ(6)-苯并[1',2',4']噻二嗪-3'-基)-5-羟基-2H-哒嗪-3-酮的新型丙型肝炎病毒NS5B聚合酶抑制剂。第3部分:2-、6-和7'-取代基的进一步优化及初步药代动力学评估。
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3446-55. doi: 10.1016/j.bmcl.2008.02.072. Epub 2008 Mar 5.
5
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones: Part 4. Optimization of DMPK properties.
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3421-6. doi: 10.1016/j.bmcl.2008.04.005. Epub 2008 Apr 4.
6
4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase.4-(1,1-二氧代-1,4-二氢-1λ6-苯并[1,4]噻嗪-3-基)-5-羟基-2H-哒嗪-3-酮作为丙型肝炎病毒NS5B聚合酶的有效抑制剂。
Bioorg Med Chem Lett. 2008 Aug 15;18(16):4628-32. doi: 10.1016/j.bmcl.2008.07.014. Epub 2008 Jul 10.
7
5,5'- and 6,6'-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.5,5'-和 6,6'-二烷基-5,6-二氢-1H-吡啶-2-酮作为 HCV NS5B 聚合酶的有效抑制剂。
Bioorg Med Chem Lett. 2009 Nov 1;19(21):6047-52. doi: 10.1016/j.bmcl.2009.09.051. Epub 2009 Sep 17.
8
Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.六氢吡咯并和六氢-1H-吡啶并[1,2-b]哒嗪-2-酮作为丙型肝炎病毒NS5B聚合酶的强效抑制剂。
Bioorg Med Chem Lett. 2008 Sep 15;18(18):5002-5. doi: 10.1016/j.bmcl.2008.08.017. Epub 2008 Aug 9.
9
Combined 3D-QSAR, molecular docking, molecular dynamics simulation, and binding free energy calculation studies on the 5-hydroxy-2H-pyridazin-3-one derivatives as HCV NS5B polymerase inhibitors.基于 HCV NS5B 聚合酶抑制剂的 5-羟基-2H-哒嗪-3-酮衍生物的三维定量构效关系、分子对接、分子动力学模拟和结合自由能计算研究的综合报告。
Chem Biol Drug Des. 2014 Jan;83(1):89-105. doi: 10.1111/cbdd.12203. Epub 2013 Oct 4.
10
Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.吡咯并[1,2 - b]哒嗪 - 2 - 酮作为丙型肝炎病毒NS5B聚合酶的强效抑制剂。
Bioorg Med Chem Lett. 2008 Jun 15;18(12):3616-21. doi: 10.1016/j.bmcl.2008.04.066. Epub 2008 May 1.

引用本文的文献

1
QSAR study of C allosteric binding site of HCV NS5B polymerase inhibitors by support vector machine.QSAR 研究丙型肝炎病毒 NS5B 聚合酶抑制剂的变构结合位点的支持向量机。
Mol Divers. 2011 Aug;15(3):645-53. doi: 10.1007/s11030-010-9283-0. Epub 2010 Oct 8.