通过晚期丝氨酸连接实现基于钙依赖性抗生素 CDA3a 的汇聚合成及其具有改善抗菌活性的类似物。
Convergent Synthesis of Calcium-Dependent Antibiotic CDA3a and Analogues with Improved Antibacterial Activity via Late-Stage Serine Ligation.
机构信息
Department of Chemistry, State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong, P. R. China.
Department of Infectious Diseases Public Health, Jockey Club College of Veterinary Medicine and Life Sciences, The City University of Hong Kong, Kowloon, Kowloon, Hong Kong, P. R. China.
出版信息
Org Lett. 2020 Jun 19;22(12):4749-4753. doi: 10.1021/acs.orglett.0c01544. Epub 2020 Jun 2.
A convergent synthesis via the late-stage serine ligation of naturally occurring calcium-dependent antibiotic CDA3a and its analogues has been developed, which allowed us to readily synthesize the analogues with the variation on the lipid tail. Some analogues were found to show 100-500-fold higher antimicrobial activity than the natural compound CDA3a against drug resistant bacteria. This study will enhance our understanding of CDA3a and provide valuable antibacterial lead candidates for further development.
已经开发出一种通过天然存在的钙依赖性抗生素 CDA3a 及其类似物的晚期丝氨酸连接的会聚合成方法，这使我们能够轻松合成带有脂质尾巴变化的类似物。一些类似物被发现对耐药菌的抗菌活性比天然化合物 CDA3a 高 100-500 倍。这项研究将增强我们对 CDA3a 的理解，并为进一步开发提供有价值的抗菌先导候选物。
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