Replacements for lysine in l-seryl- l-lysyl dipeptide amide inhibitors of candida albicans myristoyl-CoA:protein N-myristoyltransferase
A survey of potential cyclic and acyclic lysine replacements in known l-seryl- l-lysyl dipeptide inhibitors of C. albicans NMT identified the thioether 16 and glycinamide 18 as submicromolar inhibitors of C. albicans NMT, which retained good selectivity over the human enzyme. All of the heterocyclic...
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Published in | Bioorganic & medicinal chemistry letters Vol. 7; no. 3; pp. 379 - 382 |
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Main Authors | , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
04.02.1997
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | A survey of potential cyclic and acyclic lysine replacements in known
l-seryl-
l-lysyl dipeptide inhibitors of
C. albicans NMT identified the thioether
16 and glycinamide
18 as submicromolar inhibitors of
C. albicans NMT, which retained good selectivity over the human enzyme. All of the heterocyclic lysine mimetics that were examined exhibited dramatically weaker affinity with the fungal enzyme.
A potent and selective peptidomimetic inhibitor
18 has been identified where the basic lysine side chain has been replaced with a less basic glycinamide. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(97)00030-9 |