Aryloxyacetic esters structurally related to α-Asarone as potential antifungal agents

Abstract

A series of aryloxyacetic ester analogues 8-13 was synthesized based on the potential pharmacophores of the antifungal agents a-Asarone (1) and 2-5. Their antifungal activity was tested in vitro for their growth inhibitory activities against pathogenic fungi. The in vitro antifungal evaluation of these alkyl and aryl esters shows that derivatives 10 displayed the highest antifungal and fungicidal activities against Cryptococcus neoformans and C. gattii. These results support the idea that the phenoxyacetic frame is a potent pharmacophore for the design of potential antifungal drugs.

Baeyer-Villiger-Including Domino Two-Step Oxidations of β-O-Substituted Primary Alcohols: Reflection of the Migratory Aptitudes of O-Substituted Alkyl Group in the Outcome of the Reaction

“…Accordingly, we tested a number of additional primary alcohol substrates in the domino oxidation reaction (Table 1). 2-phenoxyethanol (1a), for instance, exhibited slow conversion into both the corresponding hemiacetal formate 2a and the corresponding carboxylic acid 3a [36] (entry 1). In order to achieve full consumption of the starting material, the TEMPO/TBAB loading should be increased to 5 molar %, while that of mCPBA to 6.6 equiv.…”