Pleuromutilin derivatives having a purine ring. Part 1: new compounds with promising antibacterial activity against resistant Gram-positive pathogens.
In the course of our research aimed at the discovery of metabolic stable pleuromutilin derivatives with more potent antibacterial activity against Gram-positive pathogens than previous analogues, a series of compounds bearing a purine ring were prepared and evaluated. From SAR studies, we identified two promising compounds 85 and 87, which have excellent in vitro activity against a number of Gram-positive pathogens, including existing drug-resistant strains, and potent in vivo efficacy.
Hirokawa
Yoshimi
Y
Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, Enoki 33-94, Suita 564-0053, 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 / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D024881:Drug Resistance, Bacterial; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011083:Polycyclic Compounds; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000097567:Pleuromutilins
D000900:Anti-Bacterial Agents; D004224:Diterpenes; D011083:Polycyclic Compounds; D011687:Purines; D000097567:Pleuromutilins; C030985:purine