Pleuromutilin derivatives having a purine ring. Part 2: influence of the central spacer on the antibacterial activity against Gram-positive pathogens.
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.
Hirokawa
Yoshimi
Y
Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co, Ltd, Enoki, Suita, Japan.
Kinoshita
Hironori
H
Tanaka
Tomoyuki
T
Nakamura
Takanori
T
Fujimoto
Koichi
K
Kashimoto
Shigeki
S
Kojima
Tsuyoshi
T
Kato
Shiro
S
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D004224:Diterpenes / Q000737:chemistry; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D011083:Polycyclic Compounds; D011687:Purines / Q000737:chemistry*; D012995:Solubility; D013329:Structure-Activity Relationship; D000097567:Pleuromutilins
D000900:Anti-Bacterial Agents; D004224:Diterpenes; D011083:Polycyclic Compounds; D011687:Purines; D000097567:Pleuromutilins; C030985:purine