Skip to main content

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

Buy Article:

$63.00 plus tax (Refund Policy)

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; analgesic and antithrombotic properties; antiinflammatory; molecular hybridization and bioisosterism in drug design

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986706775197881

Affiliations: Laboratorio de Avaliacao e Síntese de Substancias Bioativas (LASSBio), Faculdade de Farmacia, Universidade Federal do Rio de Janeiro, PO Box 68006, ZIP CODE 21944-971, Rio de Janeiro, RJ, Brazil.

Publication date: January 1, 2006

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

Access Key

Free Content
Free content
New Content
New content
Open Access Content
Open access content
Partial Open Access Content
Partial Open access content
Subscribed Content
Subscribed content
Free Trial Content
Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more