Asymmetric Total Synthesis Enables Discovery of Antibacterial Activity of Siladenoserinols A and H.
Org Lett. 2019 Nov 20;:
Authors: Márquez-Cadena MA, Ren J, Ye W, Qian P, Tong R
Siladenoserinols A and H were found to show moderate inhibitory activity toward p53-Hdm2 interactions. Our total synthesis allowed us to further examine their bioactivities, which revealed that (i) siladenoserinols A and H were not cytotoxic against cancer cell lines and (ii) siladenoserinol A and its desulfamate analogue exhibited significant antibacterial activity against Gram-positive bacteria including MRSA. Our studies demonstrate that siladenoserinols are a promising new class of bactericidal Gram-positive antibiotics without hemolytic activity.
PMID: 31747295 [PubMed - as supplied by publisher]