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Rhodanine-3-acetic acid derivatives as inhibitors of fungal protein mannosyl transferase 1 (PMT1).

Abstract：

:The first inhibitors of fungal protein: mannosyl transferase 1 (PMT1) are described. They are based upon rhodanine-3-acetic acid and several compounds have been identified, for example, 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]methylene]-4-oxo-2-thioxo-3-thiazolidineacetic acid (5a), which inhibit Candida albicans PMT1 with IC(50)s in the range 0.2-0.5 microM. Members of the series are effective in inducing changes in morphology of C. albicans in vitro that have previously been associated with loss of the transferase activity. These compounds could serve as useful tools for studying the effects of protein O-mannosylation and its relevance in the search for novel antifungal agents.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Orchard MG,Neuss JC,Galley CM,Carr A,Porter DW,Smith P,Scopes DI,Haydon D,Vousden K,Stubberfield CR,Young K,Page M

doi

10.1016/j.bmcl.2004.05.050

subject

Has Abstract

pub_date

2004-08-02 00:00:00

pages

3975-8

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960894X04007000

journal_volume

14

pub_type

杂志文章

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