Abstract
Inhibition of cyclooxygenase is the way of therapeutic activities for anti-inflammatory pharmaceuticals. Serum albumins are the major soluble protein able to bind and transport a variety of exogenous and endogenous ligands, including hydrophobic pharmaceuticals. In this study, a novel N-substituted 1H-pyrrolo[3–c]pyridine-1,3(2H)-diones derivatives were synthesized and biologically evaluated for their inhibitory activity against cyclooxygenases and interactions with BSA. In vitro, COX-1 and COX-2 inhibition assays were performed. Interaction with BSA was studied by fluorescence spectroscopy and circular dichroism measurement. The molecular docking study was conducted to understand the binding interaction of compounds in the active site of cyclooxygenases and BSA. The result of the COX-1 and COX-2 inhibitory studies revealed that all the compounds potentially inhibited COX-1 and COX-2. The IC50 value was found similar to meloxicam. The intrinsic fluorescence of BSA was quenched by tested compounds due to the formation of A/E–BSA complex. The results of the experiment and molecular docking confirmed the main interaction forces between studied compounds and BSA were hydrogen bonding and van der Waals force.
Highlights
Derivatives of 3,4-pyridinedicarboximides have been interesting for many years
N-(2,6-dimethylphenyl)-3,4- pyridinedicarboximide is active against MES (Maximal Electroshock Seizures) and appears to be a promising compound for the design of anticonvulsant drugs [1]
COX-1 and COX-2 enzymes aim of this work was the investigation of the synthesized compounds for their potencies to inhibit and study interaction with bovine albumin. with bovine serum albumin
Summary
Derivatives of 3,4-pyridinedicarboximides have been interesting for many years. Most of them show various kinds of biological activities. The 3,4-pyridinedicarboximide was a base compound in the design and synthesis of azaisoindolinone derivatives with a lipophilic chain. COX-1 and COX-2 are the therapeutic targets for including ibuprofen, ibuprofen, naproxen, naproxen, diclofenac, diclofenac, or or piroxicam, piroxicam, as as well well as as newer newer COX-2 Through their anti-inflammatory, anti-pyretic, and analgesic activities, they represent a choice treatment their anti-inflammatory, anti-pyretic, and analgesic activities, choice treatment in in various inflammatory diseases such as arthritis, rheumatisms as well as relieving the painsthe of everyday various inflammatory diseases such as arthritis, rheumatisms as well as relieving pains of life [7,8]. No activity was found, onlyeffect the potential analgesic was investigation of the synthesized compounds for their potencies to inhibit. COX-2 enzymes aim of this work was the investigation of the synthesized compounds for their potencies to inhibit and study interaction with bovine albumin.
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