| Autor: |
Devadas, B., Freeman, S. K., McWherter, C. A., Kishore, N. S., Lodge, J. K., Jackson-Machelski, E., Gordon, J. I., Sikorski, J. A. |
| Zdroj: |
Journal of Medicinal Chemistry; March 12, 1998, Vol. 41 Issue: 6 p996-1000, 5p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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