New β-glucan inhibitors as antifungal drugs.

Abstract:

INTRODUCTION:New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the commercially available lipopeptide/echinocandin agents caspofungin, micafungin and anidulafungin. AREA COVERED:This review covers applications disclosing compound classes that include synthetic pyridazinone analogs, bicyclic heteroaryl ring compounds, aniline derivates, and semi-synthetic echinocandin and enfumafungin derivatives. MK-3118 is an analog of the natural product enfumafungin that, in particular, shows promise as it has a spectrum of activity comparable with caspofungin but has the advantageous property of oral bioavailability. EXPERT OPINION:The diversity of chemical classes in the present review, which have demonstrable activity against β-glucan and the prospect of oral bioavailability, offers hope that safe and effective antifungal drugs will emerge and be commercialized. Of particular note, the Merck compound MK-3118, with solid evidence of efficacy based on preclinical data, has moved into clinical trials.

journal_name

Expert Opin Ther Pat

authors

Hector RF,Bierer DE

doi

10.1517/13543776.2011.603899

subject

Has Abstract

pub_date

2011-10-01 00:00:00

pages

1597-610

issue

10

eissn

1354-3776

issn

1744-7674

journal_volume

21

pub_type

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