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.
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http://dx.doi.org/10.1016/j.bioorg.2014.05.004 | DOI Listing |
Sci Rep
January 2025
Markanda National College, District-Kurukshetra, Shahabad (M), 136135, Haryana, India.
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 PDFFuture Med Chem
January 2025
Department of Chemistry, Faculty of Science, Ain Shams University, Cairo, Egypt.
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.
ACS Pharmacol Transl Sci
January 2025
Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, 48149 Münster, Germany.
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 PDFPest Manag Sci
January 2025
College of Materials and Chemistry and School of Plant Protection, Anhui Agricultural University, Hefei, China.
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.
Bioorg Chem
January 2025
Department of General Surgery, the Second Xiang-Ya Hospital, Central South University, Changsha 410011 China. Electronic address:
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.
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