Selective Activation of Antifungal Prodrugs

抗真菌前药的选择性激活

• 批准号: 6480499
• 负责人: SEAN O'MALLEY
• 金额: $ 28.74万
• 依托单位: HAWAII BIOTECH, INC.
• 依托单位国家: 美国
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-08-15 至 2005-08-14
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6480499
• 关键词: Candida albicans; amphotericin B; antifungal agents; aspartic endopeptidases; candidiasis; chemical conjugate; drug design /synthesis /production; drug metabolism; drug screening /evaluation; laboratory mouse; prodrugs

DESCRIPTION (Provided by applicant): The proposed research will investigate the feasibility of utilizing inherent properties of the infection site as a means to activate antifungal prodrugs selectively. Prodrug derivatives of an antifungal agent will be prepared and tested for their susceptibility to activation by conditions present at infection sites of C. albicans. Test compounds will be analyzed both in vitro and in vivo to determine their selectivity for the fungal infection. Promising leads will be those compounds which are both easily activated by these conditions and are resistant to activation in the normal mammalian physiological environment. Phase II will optimize the prodrug design based on our lead candidates and take this second generation design into preclinical testing.

描述（由申请人提供）：拟议的研究将调查 利用感染部位的固有特性作为一种手段的可行性 选择性地激活抗真菌前药。前药衍生物 抗真菌剂将得到准备并测试其易感性 在白色念珠菌感染部位存在的条件激活。测试 将在体外和体内分析化合物，以确定它们 真菌感染的选择性。有希望的铅将是这些化合物 这些条件都很容易激活，并且对 正常哺乳动物生理环境中的激活。第二阶段 根据我们的铅候选人优化前药设计，然后第二次 临床前测试的生成设计。