Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myr

Details Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myr Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myr

1997-03-24

1999-08-24

Tsang, Cecilia J.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Tripeptides, e.g., tripeptide thyroliberin , etc.

514 18, 514 19, 562567, 562562, A61K 3806

Patent

active

059426004

ABSTRACT:
Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: ##STR1## wherein R.sup.1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R.sup.2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C. albicans with little effect on human NMT enzyme and thus would be useful in treating C. albicans fungal infections in humans.

REFERENCES:
patent: 5486503 (1996-01-01), Oppenheim
Devadas, J. Med. Chem 41, 996, 1998.

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