Estratégia de simplificação molecular no planejamento racional de fármacos: a descoberta de novo agente cardioativo

Abstract

Recebido em 24/1/02; aceito em 17/4/02 STRATEGY OF MOLECULAR SIMPLIFICATION IN RATIONAL DRUG DESIGN: THE DISCOVERY OF A NEW CARDIOACTIVE AGENT. In this article are described examples of the successful use of molecular simplification strategy in the discovery of new drugs from bioactive natural products and synthetic compounds. The discovery of a new cardiotonic derivative (37, 2-thienylidene-3,4-methylenedioxybenzoylhydrazine; LASSBio-294), efficiently synthesized from Brazilian natural product and structurally designed by molecular simplification of active pyridazinone compounds reported in the literature, is described. A brief description of the pharmacological profile of this new cardiotonic lead-compound, belonging to the N-acylhydrazone (NAH) class, is also reported herein.