دورية
Total synthesis and antifungal evaluation of cyclic aminohexapeptides
| العنوان: | Total synthesis and antifungal evaluation of cyclic aminohexapeptides |
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| المؤلفون: | Klein, Larry L., Li, Leping, Chen, Hui-Ju, Curty, Cynthia B., DeGoey, David A., Grampovnik, David J., Leone, Christina L., Thomas, Sheela A., Yeung, Clinton M., Funk, Kenneth W., Kishore, Vimal, Lundell, Edwin O., Wodka, Dariusz, Meulbroek, Jon A., Alder, Jeffrey D., Nilius, Angela M., Lartey, Paul A., Plattner, Jacob J. |
| المصدر: | Bioorganic & Medicinal Chemistry; July 2000, Vol. 8 Issue: 7 p1677-1696, 20p |
| مستخلص: | The need for new therapies to treat systemic fungal infections continues to rise. Naturally occurring hexapeptide echinocandin B (1) has shown potent antifungal activity via its inhibition of the synthesis of β-1,3 glucan, a key fungal cell wall component. Although this series of agents has been limited thus far based on their physicochemical characteristics, we have found that the synthesis of analogues bearing an aminoproline residue in the ‘northwest’ position imparts greatly improved water solubility (>5 mg/mL). The synthesis and structure–activity relationships (SAR) based on whole cell and upon in vivo activity of the series of compounds are reported. |
| قاعدة البيانات: | Supplemental Index |
Full Text Finder | تدمد: | 09680896 14643391 |
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| DOI: | 10.1016/S0968-0896(00)00097-3 |