The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 24, 1999

Filed:

Mar. 24, 1997
Applicant:
Inventors:

James A Sikorski, Des Peres, MO (US);

Balekudru Devadas, Chesterfield, MO (US);

Daniel P Getman, Chesterfield, MO (US);

David L Brown, Chesterfield, MO (US);

Srinivasan Nagarajan, Chesterfield, MO (US);

Mark E Zupec, O'Fallon, IL (US);

Jeffrey I Gordon, St. Louis, MO (US);

Assignee:

G. D. Searle & Co., Chicago, IL (US);

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K / ;
U.S. Cl.
CPC ...
530331 ; 514 18 ; 514 19 ; 562567 ; 562562 ;
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.


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