• 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

合成及吡喹酮衍生物对日本血吸虫活性的 SAR 研究。

Synthesis and SAR studies of praziquantel derivatives with activity against Schistosoma japonicum.

机构信息

School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China.

出版信息

Molecules. 2013 Jul 31;18(8):9163-78. doi: 10.3390/molecules18089163.

DOI:10.3390/molecules18089163
PMID:23912271
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6269691/
Abstract

The synthesis and structure-activity relationship (SAR) studies of praziquantel derivatives with activity against adult Schistosoma japonicum are described. Several of them showed better worm killing activity than praziquantel and could serve as leads for further optimization.

摘要

描述了具有抗日本血吸虫成虫活性的吡喹酮衍生物的合成及构效关系（SAR）研究。其中一些化合物的杀蠕虫活性优于吡喹酮，可作为进一步优化的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/fee8412448e9/molecules-18-09163-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/fca26be71163/molecules-18-09163-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/233ee9db7935/molecules-18-09163-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/fee8412448e9/molecules-18-09163-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/fca26be71163/molecules-18-09163-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/233ee9db7935/molecules-18-09163-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b430/6269691/fee8412448e9/molecules-18-09163-g003.jpg

相似文献

1
Synthesis and SAR studies of praziquantel derivatives with activity against Schistosoma japonicum.合成及吡喹酮衍生物对日本血吸虫活性的 SAR 研究。
Molecules. 2013 Jul 31;18(8):9163-78. doi: 10.3390/molecules18089163.
2
Development of chiral praziquantel analogues as potential drug candidates with activity to juvenile Schistosoma japonicum.手性吡喹酮类似物作为对日本血吸虫幼虫具有活性的潜在候选药物的开发。
Bioorg Med Chem Lett. 2014 Sep 1;24(17):4223-6. doi: 10.1016/j.bmcl.2014.07.039. Epub 2014 Jul 22.
3
Praziquantel derivatives exhibit activity against both juvenile and adult Schistosoma japonicum.吡喹酮衍生物对日本血吸虫的幼体和成虫均有活性。
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1587-90. doi: 10.1016/j.bmcl.2011.12.133. Epub 2012 Jan 4.
4
Praziquantel derivatives with antischistosomal activity: aromatic ring modification.具有抗血吸虫活性的吡喹酮衍生物：芳环修饰。
Chem Biol Drug Des. 2013 Aug;82(2):216-25. doi: 10.1111/cbdd.12153. Epub 2013 Jun 29.
5
Pharmacological and immunological effects of praziquantel against Schistosoma japonicum: a scoping review of experimental studies.吡喹酮抗日本血吸虫的药理和免疫作用：实验研究的范围综述。
Infect Dis Poverty. 2018 Feb 7;7(1):9. doi: 10.1186/s40249-018-0391-x.
6
Design, synthesis and biological evaluation of praziquantel and endoperoxide conjugates as antischistosomal agents.吡喹酮与内过氧化物缀合物作为抗血吸虫药物的设计、合成及生物学评价
Future Med Chem. 2015;7(6):713-25. doi: 10.4155/fmc.15.20.
7
Synthesis of fluorescent derivatives of praziquantel: cell-imaging and interaction with Schistosoma japonicum cercariae.吡喹酮荧光衍生物的合成：细胞成像及与日本血吸虫尾蚴的相互作用。
Org Biomol Chem. 2013 Sep 28;11(36):5989-93. doi: 10.1039/c3ob41348a.
8
Is there a reduced sensitivity of dihydroartemisinin against praziquantel-resistant Schistosoma japonicum?双氢青蒿素对吡喹酮耐药日本血吸虫是否敏感性降低？
Parasitol Res. 2014 Jan;113(1):223-8. doi: 10.1007/s00436-013-3647-1. Epub 2013 Oct 22.
9
[Studies on resistance of Schistosoma to praziquantel XIII resistance of Schistosoma japonicum to praziquantel is experimentally induced in laboratory].[日本血吸虫对吡喹酮的抗性研究 XIII 日本血吸虫对吡喹酮的抗性在实验室中经实验诱导产生]
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi. 2011 Dec;23(6):605-10.
10
[Coadministration of pyquiton and furapromidum in the treatment of experimental schistosomiasis japonica (author's transl)].吡喹酮与呋喃丙胺合并应用治疗实验性日本血吸虫病（作者译）
Yao Xue Xue Bao. 1981 Feb;16(2):149-52.

引用本文的文献

1
CXCR6 recruits Th2 cells and promotes liver fibrosis in schistosomiasis japonica.趋化因子受体6招募辅助性T细胞2并促进日本血吸虫病中的肝纤维化。
Hepatol Commun. 2025 Aug 26;9(9). doi: 10.1097/HC9.0000000000000784. eCollection 2025 Sep 1.
2
-Schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis.可见光光氧化还原催化合成的含1,2,5-恶二嗪烷化合物的血吸虫活性及药物代谢动力学性质
RSC Med Chem. 2024 Sep 26;15(12):4001-10. doi: 10.1039/d4md00599f.
3
Circulating cell-free DNA as a biomarker for diagnosis of Schistosomiasis japonica.

本文引用的文献

1
3-oxoacyl-ACP reductase from Schistosoma japonicum: integrated in silico-in vitro strategy for discovering antischistosomal lead compounds.日本血吸虫 3-氧酰基辅酶 A 还原酶：发现抗血吸虫先导化合物的计算-体外综合策略。
PLoS One. 2013 Jun 7;8(6):e64984. doi: 10.1371/journal.pone.0064984. Print 2013.
2
Praziquantel derivatives with antischistosomal activity: aromatic ring modification.具有抗血吸虫活性的吡喹酮衍生物：芳环修饰。
Chem Biol Drug Des. 2013 Aug;82(2):216-25. doi: 10.1111/cbdd.12153. Epub 2013 Jun 29.
3
[Schistosomiasis situation in People's Republic of China in 2011].
循环游离 DNA 作为日本血吸虫病诊断的生物标志物。
Parasit Vectors. 2024 Mar 6;17(1):114. doi: 10.1186/s13071-024-06203-x.
4
Single-cell RNA sequencing reveals a peripheral landscape of immune cells in Schistosomiasis japonica.单细胞 RNA 测序揭示日本血吸虫病外周免疫细胞全景。
Parasit Vectors. 2023 Oct 10;16(1):356. doi: 10.1186/s13071-023-05975-y.
5
Metabolism of (R)-Praziquantel versus the Activation of a Parasite Transient Receptor Potential Melastatin Ion Channel.（R）-吡喹酮的代谢与寄生虫瞬时受体电位 melastatin 离子通道的激活。
ChemMedChem. 2023 Sep 15;18(18):e202300140. doi: 10.1002/cmdc.202300140. Epub 2023 Jun 15.
6
Medicinal chemistry perspectives of 1,2,3,4-tetrahydroisoquinoline analogs - biological activities and SAR studies.1,2,3,4-四氢异喹啉类似物的药物化学视角——生物活性及构效关系研究
RSC Adv. 2021 Mar 29;11(20):12254-12287. doi: 10.1039/d1ra01480c. eCollection 2021 Mar 23.
7
Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?人类血吸虫病的化疗：我们已经取得了哪些进展？有什么新进展？我们从这里将走向何方？
RSC Med Chem. 2020 Apr 6;11(4):455-490. doi: 10.1039/d0md00062k. eCollection 2020 Apr 1.
8
(S)-(+)-cis-4'-Benzyl-oxypraziquantel.（S）-（+）-顺式-4'-苄氧基吡喹酮
Acta Crystallogr Sect E Struct Rep Online. 2013 Nov 30;69(Pt 12):o1835-6. doi: 10.1107/S1600536813031735.
[2011年中华人民共和国血吸虫病疫情]
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi. 2012 Dec;24(6):621-6.
4
Drugs for treating Schistosoma mansoni infection.用于治疗曼氏血吸虫感染的药物。
Cochrane Database Syst Rev. 2013 Feb 28;2013(2):CD000528. doi: 10.1002/14651858.CD000528.pub2.
5
Anthelmintic activity of the natural compound (+)-limonene epoxide against Schistosoma mansoni.天然化合物（+）-柠檬烯环氧化物对曼氏血吸虫的驱虫活性。
Planta Med. 2013 Mar;79(3-4):253-8. doi: 10.1055/s-0032-1328173. Epub 2013 Feb 13.
6
Natural products as a source for treating neglected parasitic diseases.天然产物作为治疗被忽视寄生虫病的来源。
Int J Mol Sci. 2013 Feb 6;14(2):3395-439. doi: 10.3390/ijms14023395.
7
[(η(6)-Praziquantel)Cr(CO)3] derivatives with remarkable in vitro anti-schistosomal activity.具有显著抗血吸虫活性的 [(η(6)-Praziquantel)Cr(CO)3] 衍生物。
Chemistry. 2013 Feb 11;19(7):2232-5. doi: 10.1002/chem.201204291. Epub 2013 Jan 7.
8
Susceptibility or resistance of praziquantel in human schistosomiasis: a review.吡喹酮治疗人体血吸虫病的敏感性或耐药性：综述。
Parasitol Res. 2012 Nov;111(5):1871-7. doi: 10.1007/s00436-012-3151-z. Epub 2012 Oct 7.
9
Ferrocenyl derivatives of the anthelmintic praziquantel: design, synthesis, and biological evaluation.驱虫药吡喹酮的二茂铁衍生物：设计、合成与生物评价。
J Med Chem. 2012 Oct 25;55(20):8790-8. doi: 10.1021/jm301077m. Epub 2012 Oct 10.
10
Fungal transformation and schistosomicidal effects of pimaradienoic acid.表松烯二酸的真菌转化和杀血吸虫效果。
Chem Biodivers. 2012 Aug;9(8):1465-74. doi: 10.1002/cbdv.201100336.