934619-01-9Relevant articles and documents
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents
Flipo, Marion,Beghyn, Terence,Leroux, Virginie,Florent, Isabelle,Deprez, Benoit P.,Deprez-Poulain, Rebecca F.
, p. 1322 - 1334 (2007)
Proteases that are expressed during the erythocytic stage of Plasmodium falciparum are newly explored drug targets for the treatment of malaria. We report here the discovery of potent inhibitors of PfA-M1, a metallo- aminopeptidase of the parasite. These
Hydroxamates: Relationships between structure and plasma stability
Flipo, Marion,Charton, Julie,Hocine, Akila,Dassonneville, Sandrine,Deprez, Benoit,Deprez-Poulain, Rebecca
supporting information; 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.