The series of bioisosteric analogs 9-17 were designed based on the potential pharmacophores of the highly hypolipidemic agents, a-asarone (1), and fibrates such as clofibrate (2) and fenofibrate (3). These compounds are characterized by their simplicity, in terms of functional group diversity, because most of them are phenoxyacetic acids or their methyl and ethyl esters monosubstituted by an ethyl side-chain at the ortho, meta, and para positions of the benzene ring. Despite this structural simplicity, these derivatives exhibited potent hypocholesterolemic activity, lowering the mice serum cholesterol and low-density lipoprotein cholesterol levels up to 40% at the lowest dose of 25 mg/kg. These results supported the concept that the phenoxyacetic frame and the ethyl side-chain can be considered as potent pharmacophores for the preparation of potential hypocholesterolemic drugs. Drug Dev. Res. 64:28-40, 2005.
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.
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