Abstract

In this minireview, we refer to recent results as far as the Platelet Activating Factor (PAF) inhibitors are concerned. At first, results of organic compounds (natural and synthetic ones and specific and nonspecific) as inhibitors of PAF are reported. Emphasis is given on recent results about a new class of the so-called metal-based inhibitors of PAF. A small library of 30 metal complexes has been thus created; their anti-inflammatory activity has been further evaluated owing to their inhibitory effect against PAF in washed rabbit platelets (WRPs). In addition, emphasis has also been placed on the identification of preliminary structure-activity relationships for the different classes of metal-based inhibitors.

Highlights

  • This work was motivated by the fact that a comprehensive survey on metal-based potent inhibitors of Platelet Activating Factor (PAF) as active anti-inflammatory drugs has not been previously described in the literature

  • The present minireview describes the latest results on the application of a series of metal complexes with diverse structures and different metal cores as PAF inhibitors in WPRs, a new class of the so-called metal-based inhibitors of PAF

  • For the rhodium complexes, a straightforward relationship has been addressed, denoting that the square planar organometallic Rh(I) complexes display an inhibitory effect at the nanomolar level than the Rh(III) congeners

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Summary

Introduction

This work was motivated by the fact that a comprehensive survey on metal-based potent inhibitors of PAF as active anti-inflammatory drugs has not been previously described in the literature It is the aim of this microreview to reveal the critical role of the metal center and of the molecular structure (different coordination geometries) of the relevant metal complexes within this series of new metal-based potent inhibitors of PAF. Biological results of these compounds are reviewed and added to the dataset base of inorganic metalbased anti-inflammatory drugs. The structural characteristics and the biological activity against PAF, of different classes of metal-based inhibitors, are presented

General Characteristics of the Platelet Activating Factor
Organic PAF Inhibitors
Inorganic Metal-Based Inhibitors
Rhodium Complexes with Bidentate Nitrogen Containing Ligands
PAFR extracellular domain
Findings
Conclusions
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