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Química Nova

Print version ISSN 0100-4042On-line version ISSN 1678-7064

Abstract

PEREIRA, Dárcio Gomes. The importance of metabolism in drug design. Quím. Nova [online]. 2007, vol.30, n.1, pp.171-177. ISSN 0100-4042.  http://dx.doi.org/10.1590/S0100-40422007000100029.

It is widely recognized that pharmacokinetic optimization needs to be addressed early in drug discovery to reduce the high failure rate in bringing drugs to market. Poor absorption, too short duration of action due to high elimination rate, or the presence of active metabolites are examples of properties that can potentially lead to unsuccessful clinical programmes. Here I describe a brief overview of advantages and molecular strategies for improving metabolic and pharmacokinetic properties applied to the discovery of fluconazol, b-blockers, ritonavir and ezetimibe and to the development of the prodrugs enalapril and bambuterol.

Keywords : drug metabolism; drug design; structure-metabolism relationship.

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