In vitro antifungal activity of 2‐(2′‐hydroxy‐5′‐aminophenyl)benzoxazole in Candida spp. strains

Abstract

The development of azole antifungals has allowed for the treatment of several fungal infections. However, the use of these compounds is restricted because of their hepatotoxicity or because they need to be administered together with other drugs in order to prevent resistance to monotherapy. Benzoxazole derivatives are among the most thriving molecular prototypes for the development of antifungal agents. 2-(2'-hydroxyphenyl) benzoxazoles are versatile molecules that emit fluorescence and have antibacterial, antiviral and antifungal properties. 2-(2'-hydroxy-5'-aminophenyl) benzoxazole (HAMBO) was tested against Candida yeast. The inhibition provided by HAMBO was lower than that of fluconazole, showing low antifungal activity against Candida spp., but equivalent to that of benzoxazoles tested in similar studies. HAMBO showed fungistatic activity against all analysed strains. This class of novel benzoxazole compounds may be used as template to produce better antifungal drugs.

Recent Advances in the Development of Pharmacologically Active Compounds that Contain a Benzoxazole Scaffold

“…Unfortunately,p oor activity was observed against all species of Candida,a nd the MIC values of these compounds were much higher in all cases than that of fluconazole. [65] The antifungal activity of benzoxazole derivative 45,w hich containsa1,3,4-thiadiazole and 1,3,4-oxadiazole nucleusw as also evaluated against five strains of fungi (i.e., Rhizopus oryzae, Aspergillus niger, Aspergillus flavus, Candida albicans, and Saccharomyces cerevisiae)b yu sing amphotericin Ba s astandard. [66] Unfortunately, 45 had lower activity than amphotericin B.…”

An ESIPT fluorescent probe sensitive to protein α-helix structures

“…[6][7][8][9] Stefani's group reported the use of benzazole derivatives to stain Candida albicans ATCC 10231 cells and characterize nanocapsule polymeric walls, as well as to probe rice protein and bovine serum albumin (BSA) in solutions, but the detailed mechanisms are still to be explored. [10][11][12][13][14] A large majority of membrane proteins have one or more transmembrane regions consisting of α-helices. Membrane protein levels differ from one type of cell to another, and the expression of membrane proteins also changes from normal to diseased cells.…”

Synthesis and biological activity of some novel N-dichloroacetyl-2,3-dihydrobenzoxazole derivatives

“…In particular, 2,3-dihydrobenzoxazole derivatives have attracted widespread attention owing to their diverse biological activity and medicinal uses such as antibiotics, elastase inhibitors, and Gram-positive antibacterial, antiparasitic, anti-infl ammatory, anti-stress, anti-ulcer, and anticancer agents (Sum et al , 2003 ;Daboit et al , 2009 ;Song et al , 2010 ). They have been investigated for potential use as herbicide safeners that can regulate the activity of glutathione-S -transferase (GST) which catalyzes the metabolism of herbicide via conjugation with reduced glutathione (GSH) in plant (Hatzios and Burgos , 2004 ).…”