Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogens

Y Hirokawa, H Kinoshita, T Tanaka, T Nakamura…

文献索引：Hirokawa, Yoshimi; Kinoshita, Hironori; Tanaka, Tomoyuki; Nakamura, Takanori; Fujimoto, Koichi; Kashimoto, Shigeki; Kojima, Tsuyoshi; Kato, Shiro Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 1 p. 170 - 174

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被引用次数: 20

摘要

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.