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

项目亮点：完成了药物化学优化，并测试了针对5-HLO和CyP51的化合物。合成了一种新型的抗真菌药酮康唑，并进行了放大实验。 在此期间，NCGC与NIH和校外调查人员进行了180多次积极的合作，促进了整个人类疾病范围内的药物发现工作。这些努力已经产生了100多个高通量筛选和近60个药物化学活动，为我们的合作者和一般研究社区提供了丰富的出版物和前景光明的小分子线索。此外，NCGC还承担了一些信息学挑战，以更好地利用现有的药物和疾病目标信息，并为公众提供易于获取的资源，进一步催化人类疾病新疗法的开发。

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.