新型含N-吡啶联吡唑类二聚体衍生物的合成及抗猪伪狂犬病毒(PRV)活性评价
Synthesis and Anti-porcine Pseudorabies Virus(PRV)Activity of Novel N-Pyridinium Bipyrazole Dimer Derivatives
侯学会 1姚晨 2宋锦清 3杨菲菲 3何张旭 3陈晓培 1张京玉3
作者信息
- 1. 河南牧业经济学院理学部 郑州 450046
- 2. 河南农业大学动物医学院 郑州 450046
- 3. 河南中医药大学药学院 郑州 450046
- 折叠
摘要
猪伪狂犬病毒(PRV)不仅感染多种脊椎动物,还可直接感染人类,导致神经和呼吸系统严重受损,引起了人们对PRV跨物种传播的担忧,然而,针对PRV的特异性抗病毒药物很少.运用分子拼接和电子等排的原理,设计合成了 25个含N-吡啶联吡唑类二聚体衍生物,并测试了目标化合物对PRV病毒的抑制效果.初步生物活性测试数据显示,大多数化合物在10μmol/L浓度下表现出较强的抗PRV病毒活性,且对猪源肾上皮细胞(PK-15)具有无毒性或者低毒性.此类新型含N-吡啶联吡唑类二聚体衍生物可作为潜在抗PRV病毒的先导化合物进一步优化和开发.
Abstract
The porcine pseudorabies virus(PRV)leading to severe neurological and respiratory damage can infect a wide range of vertebrates and humans,which raises concerns regarding the potential cross-species transmission of PRV.However,there is currently a lack of specific antiviral treatments available for PRV.25 dimer derivatives containing N-pyridine bipyra-zole moiety were designed and synthesized based on the principles of molecular splicing and electron isoarrangement.The inhibitory effect of the target compounds on PRV virus was assessed.Preliminary bioassay revealed that most of the com-pounds exhibited potent anti-PRV activity at a concentration of 10 μmol/L while demonstrating no or minimal toxicity towards a type of porcine kidney cell(PK-15).These novel N-pyridinium bipyrazole dimer derivatives could be regarded as anti-PRV agents for further optimization and development.
关键词
N-吡啶联吡唑/二聚体/抗猪伪狂犬病毒(PRV)活性Key words
N-pyridinium bipyrazole/dimer derivative/anti-porcine pseudorabies virus(PRV)activity引用本文复制引用
基金项目
河南省自然科学基金(202300410264)
河南省科技攻关项目(232102111051)
中国博士后科学基金(2022M721060)
出版年
2024
NETL
NSTL
万方数据