Blondelle S E, Crooks E, Ostresh J M, Houghten R A
Torrey Pines Institute for Molecular Studies, San Diego, California 92121, USA.
Antimicrob Agents Chemother. 1999 Jan;43(1):106-14. doi: 10.1128/AAC.43.1.106.
A mixture-based synthetic combinatorial library of more than 100,000 bicyclic guanidines was generated in a positional scanning format and assayed for activity against Candida albicans. Potent individual bicyclic guanidines were directly identified following the screening of the library. Time-kill curve studies indicated bactericidal activities for the individual bicyclic guanidines. These compounds also showed potent activity against Cryptococcus neoformans. These studies demonstrate the value of using mixture-based combinatorial positional scanning libraries made up of heterocyclic compounds for the rapid identification of novel classes of antifungal compounds.
构建了一个基于混合物的、包含超过100,000种双环胍的合成组合文库，采用位置扫描形式，并检测其对白色念珠菌的活性。在文库筛选后直接鉴定出了强效的单个双环胍。时间-杀菌曲线研究表明单个双环胍具有杀菌活性。这些化合物对新型隐球菌也显示出强效活性。这些研究证明了使用由杂环化合物组成的基于混合物的组合位置扫描文库来快速鉴定新型抗真菌化合物类别的价值。
