Synthesis and activities of bactobolin derivatives based on the alteration of the functionality at C-3 position.
Some derivatives of bactobolin were prepared from bactobolin (1) by radical reduction and formation of the fused azetidine ring. The derivatives proved less active than the parent antibiotic 1 against bacteria, indicating that dichloromethyl group at C-3 position play an important role in biological activity.
Adachi
H
H
Institute of Microbial Chemistry, Tokyo, Japan.
Usui
T
T
Nishimura
Y
Y
Kondo
S
S
Ishizuka
M
M
Takeuchi
T
T
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D011714:Pyrans; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000903:Antibiotics, Antineoplastic; D001578:Benzopyrans; D011714:Pyrans; C025268:bactobolin; C100221:actinobolin