Importance of the 6'-hydroxy group and its configuration for apramycin activity.
| Autor: | Mandhapati AR; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI 48202 (USA)., Shcherbakov D, Duscha S, Vasella A, Böttger EC, Crich D |
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| Jazyk: | angličtina |
| Zdroj: | ChemMedChem [ChemMedChem] 2014 Sep; Vol. 9 (9), pp. 2074-83. Date of Electronic Publication: 2014 Jul 17. |
| DOI: | 10.1002/cmdc.201402146 |
| Abstrakt: | A series of apramycin derivatives was prepared and investigated for antibacterial activity and the ability to inhibit protein synthesis in cell-free translation assays. The effect of various modifications at the 6'- and N7'-positions on antiribosomal activity is discussed in terms of their influence on drug binding to specific residues in the decoding A-site. These studies contribute to the development of a structure-activity relationship for the antibacterial activity of the apramycin class of aminoglycosides and to the future design and development of more active and less toxic antibiotics. (© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.) |
| Databáze: | MEDLINE |
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