2/11/2004
FARM2147
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