Use of 1,4-naphthoquinone derivatives as inhibitors of aspartyl protease, for treatment of infection by Candida or human immune deficiency virus

摘要

Use of 1,4-naphthoquinone derivatives (I) as inhibitors of SAP and HIV proteases. Use of 1,4-naphthoquinone derivatives of formula (I) as inhibitors of SAP and HIV proteases. [Image] R1-R4hydroxy, 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. Aureoquinone ((I) with all R groups = hydroxy) was tested for inhibition of release of the SAP protease from Candida CBS 5982. It was added once, at the start of the test and extinction measured at 450 nm. At a concentration of 50 Microg/ml, extinction was about 5% of that in a control. A further test showed that at 50 Microg/ml the same compound reduced adhesion of CBS 5982 to HeLa S3 cells to about 65% of that in a control.