Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogens |
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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: | Structural modification of the 4-piperidinethio moiety, as a spacer of the first pleuromutilin analogues 2A and 2B having a purine ring, led to discovery of the novel pleuromutilin derivatives 14B and 17B. These compounds with good solubility in water showed promising in vitro antibacterial activity against various Gram-positive bacteria including MRSA, PRSP, and VRE and have potent in vivo efficacy. |
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