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.
Medicinal Chemistry, Hoechst Marion Roussel/Aventis, Romainville, France. branislav.musicki@aventis.com
B
B
Musicki
A M
AM
Periers
P
P
Laurin
D
D
Ferroud
Y
Y
Benedetti
S
S
Lachaud
F
F
Chatreaux
J L
JL
Haesslein
A
A
Iltis
C
C
Pierre
J
J
Khider
N
N
Tessot
M
M
Airault
J
J
Demassey
C
C
Dupuis-Hamelin
P
P
Lassaigne
A
A
Bonnefoy
P
P
Vicat
M
M
Klich
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