192202-67-8Relevant academic research and scientific papers
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere
Beaulieu,Wernic,Abraham,Anderson,Bogri,Bousquet,Croteau,Guse,Lamarre,Liard,Paris,Thibeault,Pav,Tong
, p. 2164 - 2176 (2007/10/03)
A series of HIV protease inhibitors containing a novel (hydroxyethyl)amidosuccinoyl core has been synthesized. These peptidomimetic structures inhibit viral protease activity at low nanomolar concentrations (IC50 50) = 3,7-35 nM. This series of inhibitors was found to exhibit poor bioavailability (10%) in the rat, following oral administration. The synthesis and biological properties of these compounds are discussed. In addition, an X-ray structure of one of these inhibitors (23) in complex with HIV-2 protease provides insight into the binding mode of this novel class of HIV protease inhibitors.
