Using fungal naphthopyran-8,9-diones as inhibitors of aspartyl protease, useful for treatment of infection by Candida or human immune deficiency virus

摘要

Use of laccaridiones (I) as inhibitors of SAP and HIV proteases. Use of laccaridiones of formula (I) as inhibitors of SAP and HIV proteases. [Image] R1 -R3hydroxy, 1-8C alkoxy or 2-8C alkanoyloxy. ACTIVITY : Fungicide; Anti-HIV. MECHANISM OF ACTION : Inhibition of (a) aspartyl proteases and (b) adhesion of Candida to epithelial and/or endothelial cells. Laccaridione B ((I) with R1 = methoxy; R2 = hydroxy and R3 = ethoxy) was tested for inhibition of release of the SAP protease from Candida CBS 5982. It was added every 42 hours and extinction measured at 450 nm. At a concentration of 50 Microg/ml, extinction was about 7% of that in a control. A further test showed that at 50 Microg/ml the same compound had 100% inhibition of adhesion of CBS 5982 to HeLa S3 cells.