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Discovery of inhibitors of Zika virus

寨卡病毒抑制剂的发现

基本信息

批准号：
9252886
负责人：
Glen Andrew Coburn
金额：
$ 30万
依托单位：
VENATORX PHARMACEUTICALS, INC.
依托单位国家：
美国
项目类别：
财政年份：
2017
资助国家：
美国
起止时间：
2017-03-15 至 2019-02-28
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/9252886
关键词：
Aedes Affect American Americas Antiviral Agents Arboviruses Arthralgia Arthropod Vectors Automobile Driving Biological Assay Bite Brazil Caribbean region Centers for Disease Control and Prevention (U.S.)Central America Chikungunya virus Congenital Abnormality Conjunctivitis Country Culicidae Development Disease Disease Outbreaks Dose Drug Kinetics Epidemic Evaluation Exanthema Explosion Feasibility Studies Fetus Fever French Polynesia Funding Geographic Distribution Goals Guillain-Barré Syndrome Health Human Immunologics Incidence Individual Lead Libraries Link Maps Microcephaly Mothers National Institute of Allergy and Infectious Disease Neurologic Oral Penetration Pharmaceutical Chemistry Pharmaceutical Preparations Phase Population Predisposition Prevention Property Public Health Resistance Resources Risk Series Small Business Innovation Research Grant South America Structure-Activity Relationship Testing Therapeutic Time Vaccines Variant Vero Cells Viral Virus Virus Diseases Virus Inhibitors Virus Replication Visit West Nile virus World Health Organization Zika Virus authority base candidate selection cytotoxicity disorder prevention high throughput screening improved indexing inhibitor/antagonist innovation lead series male monolayer novel novel diagnostics novel therapeutics pathogen prevent programs response screening small molecule success transmission process vector mosquito viral transmission

项目摘要

PROJECT SUMMARY Novel inhibitors of Zika virus (ZIKV) are urgently needed to prevent the occurrence of virus-induced microcephaly and Guillain-Barré syndrome. The objective of this Phase I SBIR feasibility study is to identify drug-like compounds that specifically inhibit ZIKV replication. During the course of this Phase I funding period, we will execute hit finding campaign against a library of 100,000 compounds with optimal drug-like properties. Quality hits that emerge from the assay will be subjected to follow-on testing that will investigate the potency, selectivity, and mechanism of action. The most interesting of these compounds will be subjected to medicinal chemistry driven hit-to-lead to explore structure-activity relationships (SAR). The overall goal of this project is to discover one or more novel lead series which is defined as a chemotype inhibitor that demonstrates tractable SAR, potent antiviral activity against the available ZIKV strains and minimal cytotoxicity. Success in these endeavors will trigger the submission of a Phase II application that will advance the program from Early Lead Optimization through to Candidate Selection.

项目摘要寨卡病毒（ZIKV）的新型抑制剂是迫切需要的，以防止病毒诱导的寨卡病毒（ZIKV）的发生。小头畸形和格林-巴利综合征。第一阶段SBIR可行性研究的目的是确定特异性抑制ZIKV复制的药物样化合物。在第一阶段融资期间，我们将对10万种具有最佳药物性质的化合物库进行命中发现活动。将对试验中出现的质量命中进行后续检测，以研究效价，选择性和作用机制。这些化合物中最令人感兴趣的将受到药用化学驱动的命中导致探索结构-活性关系（SAR）。该项目的总体目标是发现一个或多个新的先导化合物系列，其被定义为一种化学型抑制剂，易于处理的SAR、针对可用ZIKV毒株的有效抗病毒活性和最小的细胞毒性。成功这些努力将引发提交第二阶段的申请，这将推动该计划从早期从优化到候选人选择。