Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
A new series of coumarin inhibitors of DNA gyrase B bearing a N-propargyloxycarbamate at C-3' of various 5',5'-dialkylnoviose, including RU79115, were synthesised and their antibacterial activities have been delineated. Introduction of dialkyl substituents at 5'5'-position of noviose leads to coumarin analogues with improved in vitro and in vivo antibacterial activity.
Musicki
B
B
Medicinal Chemistry, Hoechst Marion Roussel/Aventis, Romainville, France. branislav.musicki@aventis.com
Periers
A M
AM
Laurin
P
P
Ferroud
D
D
Benedetti
Y
Y
Lachaud
S
S
Chatreaux
F
F
Haesslein
J L
JL
Iltis
A
A
Pierre
C
C
Khider
J
J
Tessot
N
N
Airault
M
M
Demassey
J
J
Dupuis-Hamelin
C
C
Lassaigne
P
P
Bonnefoy
A
A
Vicat
P
P
Klich
M
M
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology*; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D006601:Hexoses / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D003374:Coumarins; D006601:Hexoses; C416353:RU 79115; C030123:coumarin