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.
Keywords: Bioactive N-acylhydrazone derivatives, antiinflammatory, analgesic and antithrombotic properties, molecular hybridization and bioisosterism in drug design
Current Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/092986706775197881 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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