Discovery of Inhibitors of Human 5-Lipoxygenase and CYP51 as Anti-Fungal Leads

人类 5-脂氧合酶和 CYP51 抑制剂作为抗真菌先导化合物的发现

• 批准号: 9205750
• 负责人: David Maloney
• 金额: $ 11.4万
• 依托单位: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/9205750
• 关键词: Discovery; Inhibitors; Human; Lipoxygenase; CYP51

Project highlights: completed Medicinal chemistry optimization and tested compounds against 5-hLO and CYP51. A modified version of antifungal agent ketaconazole was synthesized and scaled up. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.

项目亮点：完成药物化学优化，对5-hLO和CYP51的化合物进行了测试。合成了一种改性的抗真菌药酮康唑，并进行了规模化生产。