Synthesis and Evaluation of Novel anti-RSV Compounds

新型抗RSV化合物的合成与评价

• 批准号: 6833299
• 负责人: RONALD A FLEMING
• 金额: $ 10万
• 依托单位: KUCERA PHARMACEUTICAL COMPANY
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-01-15 至 2005-10-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6833299
• 关键词: Paramyxoviridae disease; antiviral agents; cell line; chemical synthesis; drug design /synthesis /production; drug screening /evaluation; laboratory rat; nonhuman therapy evaluation; respiratory infections; respiratory syncytial virus

DESCRIPTION (provided by applicant): The long-term objective of this research is to develop a safe and efficacious pharmacologic agent for the treatment of respiratory syncytial virus (RSV) infection. RSV is the most common cause of respiratory tract infection in infants and children in the United States. RSV associated infections result in up to 126,000 hospitalizations and more than 500 deaths in infants and small children each year. RSV infections are also a considerable cause of mortality and morbidity in the elderly and immunocompromised individuals. Ribavirin, the only FDA-approved drug for the treatment of severe RSV infections, has questionable efficacy and is difficult and costly for hospital intensive care staff to administer. The Kucera Pharmaceutical Company has identified a novel pharmacologic agent (KPC-15) with potent in vitro activity against RSV. This small molecular weight compound (m.w. < 500) is active against RSV and has little toxicity against normal host cells in vitro. These exciting results warrant further investigation of this compound. The aims of this project are to synthesize KPC-15 and to complete key in vitro and in vivo studies. The activity of KPC- 15 will be evaluated in an animal model of RSV infection (cotton rat) to determine its activity in vivo.

描述（由申请方提供）：本研究的长期目标是开发一种安全有效的用于治疗呼吸道合胞病毒（RSV）感染的药理学药物。RSV是美国婴儿和儿童呼吸道感染的最常见原因。RSV相关感染每年导致多达126，000例住院治疗和500多例婴儿和幼儿死亡。RSV感染也是老年人和免疫功能低下个体死亡和发病的重要原因。利巴韦林是FDA批准的唯一用于治疗严重RSV感染的药物，其疗效值得怀疑，并且对于医院重症监护人员来说难以管理且成本高昂。Kucera Pharmaceutical Company已鉴定出一种新型药理学药物（KPC-15），其对RSV具有有效的体外活性。这种小分子量化合物（m.w. <500）在体外对RSV有活性并且对正常宿主细胞几乎没有毒性。这些令人兴奋的结果保证了对该化合物的进一步研究。该项目的目的是合成KPC-15并完成关键的体外和体内研究。将在RSV感染的动物模型（棉鼠）中评价KPC-15的活性，以确定其体内活性。