Medicinal Chemistry of N-Acylhydrazones: New Lead-Compounds of Analgesic, Antiinflammatory and Antithrombotic Drugs

Title: Medicinal Chemistry of N-Acylhydrazones: New Lead-Compounds of Analgesic, Antiinflammatory and Antithrombotic Drugs

Volume: 13 Issue: 2

Author(s): Carlos A.M. Fraga and Eliezer J. Barreiro

Affiliation:

Keywords: Bioactive N-acylhydrazone derivatives, antiinflammatory, analgesic and antithrombotic properties, molecular hybridization and bioisosterism in drug design

Abstract: In this article we provide an overview on the medicinal chemistry of new bioactive N-acylhydrazone (NAH) derivatives designed through the structural optimization of N-arylhydrazone precursors, originally planned by molecular hybridization of two known 5-lipoxygenase inhibitors, i.e. CBS-1108 and BW-755c. The analgesic, antiedematogenic and platelet anti-aggregating profile of several isosteric NAH compounds was investigated by using classical in vivo and ex-vivo pharmacological assays, which allowed the identification of new potent centrally and peripherically-acting analgesic leads, new antiinflammatory agents and new antithrombotic prototypes. During this study, dozens of active NAH compounds were discovered, clarifying the structure-activity relationships for this series of derivatives and indicating the pharmacophoric character of the N-acylhydrazone moiety for its biological profile.

Cite this article as:

Fraga A.M. Carlos and Barreiro J. Eliezer, Medicinal Chemistry of N-Acylhydrazones: New Lead-Compounds of Analgesic, Antiinflammatory and Antithrombotic Drugs, Current Medicinal Chemistry 2006; 13 (2) . https://dx.doi.org/10.2174/092986706775197881