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Synthesis and biological evaluation of platensimycin analogs |
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| Authors: | Hong C. Shen Fa-Xiang Ding Sheo B. Singh Gopalakrishnan Parthasarathy Stephen M. Soisson Sookhee N. Ha Xun Chen Srinivas Kodali Jun Wang Karen Dorso James R. Tata Milton L. Hammond Malcolm MacCoss Steven L. Colletti |
| Affiliation: | 1. Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA;2. Natural Products, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA;3. Cardiovascular Diseases, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA;4. Infectious Diseases, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA |
| Abstract: | Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could potentially lead to a breakthrough in developing a new generation of antibiotics. The medicinal chemistry efforts were focused on the modification of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity. |
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