Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives

Bioorganic & Medicinal Chemistry
Paola HernándezHugo Cerecetto

Abstract

We report the design, the synthesis and the biological evaluation of the analgesic and anti-inflammatory activities of furoxanyl N-acylhydrazones (furoxanyl-NAH) by applying molecular hybridization approach. Hybrid compounds with IL-8-release inhibition capabilities were identified. Among them, furoxanyl-NAH, 17, and benzofuroxanyl-derivative, 24, together with furoxanyl-NAH derivative, 31, without IL-8 inhibition displayed both orally analgesic and anti-inflammatory activities. These hybrid derivatives do not have additional LOX- or COX-inhibition activities. For instance, LOX-inhibition by furoxanyl-NAH derivative, 42, emerged as a structural lead to develop new inhibitors. The lack of mutagenicity of the active derivatives 17, 31, and 42, allow us to propose them as candidates for further clinical studies. These results confirmed the success in the exploitation of hybridization strategy for identification of novel N-acylhydrazones (NAH) with optimized activities.

Citations

Nov 11, 2014·International Journal of Medicinal Chemistry·Anu KajalVipin Saini
Apr 10, 2014·International Journal of Molecular Sciences·Thais Regina Ferreira de MeloJean Leandro dos Santos
Oct 13, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Leandro Augusto RossetoJean Leandro Dos Santos
Jun 7, 2013·Medicinal Research Reviews·Ling ZhangCheng-He Zhou
Sep 13, 2014·Expert Opinion on Therapeutic Patents·Rodolfo do Couto MaiaCarlos Alberto Manssour Fraga
Oct 30, 2016·European Journal of Pharmacology·Amanda F CidadeRicardo Menegatti
Jul 1, 2017·Expert Opinion on Drug Discovery·Ricardo A M SerafimElizabeth I Ferreira
Jun 27, 2017·Bioorganic & Medicinal Chemistry Letters·Silvia Melchor-Doncel de la TorreFrancisco Hernández-Luis
Feb 26, 2020·Anti-cancer Agents in Medicinal Chemistry·Malavalli B SridharaDale C Gowda
Mar 7, 2020·MedChemComm·Fernanda Virginia Barreto MotaTeresinha Gonçalves da Silva
Sep 11, 2018·Bioorganic Chemistry·Chen LiHua-Li Qin

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