|Conférence Dr Michael J KELSO, Lecturer, School of Chemistry, University of Wollongong|
|Écrit par Administrator|
|Vendredi, 11 Décembre 2009 00:00|
Deux pour le prix d'une - double effet des médicaments hybrides et des prodrogues " - " Two for the Price of One − Dual Action Hybrid Drugs and Prodrugs
Vendredi 11 décembre 2009
Amphi 4 - Faculté de Médecine, 22 av. Camille Desmoulins - Brest
The goal of most drug discovery efforts is to produce an optimised small molecule that displays high potency and selectivity towards a validated therapeutic target. Improved therapeutic effects are sometimes achieved through the use of combination therapy; i.e. the co-administration of two (or more) drugs acting at different targets. Combination therapy is often sub-optimal, however, because the biodistribution and pharmacokinetics of two structurally unrelated compounds are invariably quite different, which makes it difficult to achieve therapeutic concentrations of both agents at the appropriate times within the target tissues. One strategy for overcoming these problems is to combine the two drugs into a single dual-action agent that is either: (1) a hybrid molecule that presents the key pharmacophoric features of both drugs, or (2) an inactive prodrug that is designed to release the two active agents only after some triggering reaction in vivo. Synthetic and biological results from our studies on dual action hybrids for combating drug resistant bacterial infections will be presented, along with our recent work on dual-action anti-cancer prodrugs.
|Mise à jour le Mercredi, 07 Juillet 2010 13:41|