gem-Difluorobisarylic derivatives: design, synthesis and anti-inflammatory effect.

ABSTRACT:

Introduction

New fluorinated diaryl ethers and bisarylic ketones were designed and evaluated for their anti-inflammatory effects in primary macrophages.

Methods

The synthesis of the designed molecules started from easily accessible and versatile gem-difluoro propargylic derivatives. The desired aromatic systems were obtained using Diels-Alder/aromatization sequences and this was followed by Pd-catalyzed coupling reactions and, when required, final functionalization steps. Both direct inhibitory effects on cyclooxygenase-1 or -2 activities, protein expression of cyclooxygenase-2 and nitric oxide synthase-II and the production of prostaglandin E₂, the pro-inflammatory nitric oxide and interleukin-6 were evaluated in primary murine bone marrow-derived macropha

SUBMITTER: Ayoub AJ 

PROVIDER: S-EPMC6824041 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature