Pleuromutilin derivatives having a purine ring. Part 3: Synthesis and antibacterial activity of novel compounds possessing a piperazine ring spacer |
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| Authors: | Yoshimi Hirokawa Hironori Kinoshita Tomoyuki Tanaka Takanori Nakamura Koichi Fujimoto Shigeki Kashimoto Tsuyoshi Kojima Shiro Kato |
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| Institution: | 1. Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, Enoki 33-94, Suita 564-0053, Japan;2. Pharmacology Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, 3-1-98 Kasugade Naka, Konohana-ku, Osaka 554-0022, Japan |
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| Abstract: | SAR studies on the water-soluble thioether pleuromutilin analogue 6, which has excellent in vitro and in vivo antibacterial activities, led to discovery of the novel pleuromutilin derivatives having a piperazine ring spacer. These derivatives displayed potent and well-balanced in vitro antibacterial activity against various drug-susceptible and -resistant Gram-positive bacteria. In particular, the promising pleuromutilin analogues 37 and 40 were found to exhibit strong in vivo efficacy against Staphylococcus aureus Smith. |
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