Convergent Synthesis of Calcium-Dependent Antibiotic CDA3a and Analogues with Improved Antibacterial Activity via Late-Stage Serine Ligation
作者:Delin Chen、Kathy Hiu Laam Po、Pilar Blasco、Sheng Chen、Xuechen Li
DOI:10.1021/acs.orglett.0c01544
日期:2020.6.19
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