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Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase. 1998
B Devadas, and
S K Freeman, and
C A McWherter, and
N S Kishore, and
J K Lodge, and
E Jackson-Machelski, and
J I Gordon, and
J A Sikorski
Department of Medicinal and Structural Chemistry, G. D. Searle and Company, St. Louis, Missouri 63198, USA.
A new class of biologically active nonpeptidic inhibitors of Candida albicans NMT has been synthesized starting from the octapeptide ALYASKLS-NH2 (2). The synthetic strategy entailed the preparation of novel protected Ser-Lys mimics 9 and 12 from (S)- or (R)-3-iodotyrosine and then grafting key enzyme recognition elements in a stepwise manner. Like 2, compounds 16, 17, and 18 are competitive Candida NMT inhibitors that bind to the peptide recognition site of the enzyme. Moreover, 16-18 have an affinity comparable to that of 2 even though they are devoid of peptide bonds. In contrast to 2, these nonpeptidic inhibitors exhibit antifungal activity.
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