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Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation |
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| Authors: | Doundoulakis Thomas Xiang Alan X Lira Ricardo Agrios Konstantinos A Webber Stephen E Sisson Wes Aust Robert M Shah Amit M Showalter Richard E Appleman James R Simonsen Klaus B |
| Affiliation: | Department of Medicinal Chemistry, Anadys Pharmaceuticals Inc., 3115 Merryfield Row, San Diego, CA 92121, USA. |
| Abstract: | A series of myxopyronin B analogs has been prepared via a convergent synthetic route and were tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against E. coli and S. aureus. The parent lead compound proved to be very sensitive to even small changes. Only the achiral desmethyl myxopyronin B (1a) provided enhanced potency. |
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