2/11/2004
FARM2147
28
Telithromycin
•Telithromycin, the first ketolide, was designed to overcome erythromycin A resistance within Gram (+) positive cocci and take advantage of PK improvements of clarithromycin
O
O
O
O
OCH3
O
9
6
N
R
3
O
O
D - desosamine
New chemical
class (3–keto)
active against ermR
C11–C12 carbamate
for anchoring
11
12
To avoid chemical
instability
Side chain for
improved
activity