71376-29-9Relevant academic research and scientific papers
Structure-activity relationship of cytochrome bc1 reductase inhibitor broad spectrum antifungal ilicicolin H
Singh, Sheo B.,Liu, Weiguo,Li, Xiaohua,Chen, Tom,Shafiee, Ali,Dreikorn, Sarah,Hornak, Viktor,Meinz, Maria,Onishi, Janet C.
, p. 3018 - 3022 (2013/06/26)
Ilicicolin H is a broad spectrum antifungal agent showing sub micro g/mL MICs against Candida spp., Aspergillus fumigatus and Cryptococcus spp. It is a potent inhibitor (C50 2-3 ng/mL) of the mitochondrial cytochrome bc1 reductase with over 1000-fold selectivity against rat liver cytochrome bc1 reductase. Structure-activity relationship of semisynthetic derivatives by chemical modification of ilicicolin H and its 19-hydroxy derivative produced by biotransformation have been described. Basic 4′-esters and moderately polar N- and O-alkyl derivatives retained antifungal and the cytochrome bc1 reductase activities. 4′,19-Diacetate and 19-cyclopropyl acetate retained antifungal and enzyme activity and selectivity with over 20-fold improvement of plasma protein binding.
