1193365-99-9Relevant academic research and scientific papers
Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors
Deprez-Poulain, Rebecca,Flipo, Marion,Piveteau, Catherine,Leroux, Florence,Dassonneville, Sandrine,Florent, Isabelle,Maes, Louis,Cos, Paul,Deprez, Benoit
, p. 10909 - 10917 (2013/03/14)
Malaria is a severe infectious disease that causes between 655 000 and 1.2 million deaths annually. To overcome the resistance to current drugs, new biological targets are needed for drug development. Aminopeptidase M1 (PfAM1), a zinc metalloprotease, has
Hydroxamates: Relationships between structure and plasma stability
Flipo, Marion,Charton, Julie,Hocine, Akila,Dassonneville, Sandrine,Deprez, Benoit,Deprez-Poulain, Rebecca
experimental part, p. 6790 - 6802 (2010/04/04)
Hydroxamates are valuable tools for chemical biology as well as interesting leads for medicinal chemistry. Although many hydroxamates display nanomolar activities against metalloproteases, only three hydroxamates have reached the market, among which is the HDAC inhibitor vorinostat. Failures in development are generally attributed to lack of selectivity, toxicity, or poor stability. To help medicinal chemists with respect to plasma stability, we have performed the first and preliminary study on structure-plasma stability for hydroxamates. We define some structural rules to predict or improve the plasma stability in the preclinical stage.
