1009036-85-4Relevant academic research and scientific papers
2-Oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability
Bulbule, Vivek J.,Rivas, Kasey,Verlinde, Christophe L. M. J.,Van Voorhis, Wesley C.,Gelb, Michael H.
, p. 384 - 387 (2008)
We report a series of novel inhibitors of protein farnesyl-transferase based on the 2-oxotetrahydroquinoline scaffold. We developed an efficient synthesis of these compounds. These compounds show selective inhibtion of the malaria versus human farnesyltransferase and inhibit the growth of the malaria parasite in the low nanomolar range. Some of the compounds are at least an order of magnitude more stable to metabolic degradation than the corresponding tetrahydroquinolines.
