A novel series of pyrazole derivatives were synthesized and evaluated in vivo for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Among all compounds, 5a, and 5b showed comparable anti-inflammatory activity to Nimesulide, the standard drug taken for the studies. In silico (docking) studies were carried out to investigate the theoretical binding mode of the compounds to target the cyclooxygenase (COX-2) using Autodock 4.2.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bioorg.2014.05.004DOI Listing

Publication Analysis

Top Keywords

pyrazole derivatives
8
anti-inflammatory activity
8
synthesis biological
4
biological evaluation
4
evaluation molecular
4
molecular modeling
4
modeling study
4
study pyrazole
4
derivatives selective
4
selective cox-2
4

Similar Publications

Pyrazole derivatives are aromatic heterocyclic compounds endowed with multifaceted applications. In the present study 1,3,4-trisubstituted pyrazoles derivatives have been synthesized for the purpose of studying their physical properties and their characterization was done by FTIR, H NMR and C NMR spectroscopic technique. The measurement of densities (ρ) and viscosities (η) of solutions of substituted pyrazole derivative in polar aprotic solvent i.

View Article and Find Full Text PDF

Aim: New phenyldiazene scaffold-linked heterocyclic pyrazole, pyrimidinone, pyrimidinthione, and/or triazine rings have been developed and synthesized.

Methods & Results: Cytotoxicity of our derivatives was estimated on four cancer and VERO normal cell lines targeting EGFR (epidermal growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) enzymes. Our new derivatives selectively inhibited both VEGFR-2 and EGFR as they have the essential structural requirements for inhibitors of both receptors.

View Article and Find Full Text PDF

This study presents a novel series of -acylated 1,2,4-triazol-5-amines and 1-pyrazol-5-amines, featuring a pyrazin-2-yl moiety, developed as covalent inhibitors of thrombin. These compounds demonstrated potent inhibitory activity, with derivatives and achieving IC values as low as 0.7 and 0.

View Article and Find Full Text PDF

Background: Development of novel chiral antifungal agents for effective control of plant pathogens is urgently needed. In this study, a series of pyrazol-5-yl-benzamide derivatives containing chiral oxazoline moiety were rationally designed and developed based on molecular docking.

Results: The in vitro antifungal assay results indicated that compounds (rac)-4h (R = Et), (S)-4 h (R = S-Et) and (R)-4 h (R = R-Et) exhibited remarkable antifungal activities against Valsa mali with median effective concentration (EC) values of 0.

View Article and Find Full Text PDF

The transforming growth factor β (TGF-β) type 1 receptor (ALK5) plays a key role in tumor microenvironment. Small-molecule inhibitors of TGFβR1 provides a prospective approach for the treatment of malignant tumors. In this study, a series of 4-((3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)quinoline derivatives were identified as novel, potential TGFβR1 inhibitors.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!