10.1039/c3ob41936c
The research presented in the "Organic & Biomolecular Chemistry" paper focuses on the discovery of potential anti-inflammatory drugs, specifically diaryl-1,2,4-triazoles bearing an N-hydroxyurea moiety, which serve as dual inhibitors of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). The study involves the synthesis and evaluation of a series of hybrid compounds derived from diaryl-1,2,4-triazole and hydroxamic acid or N-hydroxyurea, designed to act as novel anti-inflammatory agents. The synthesized compounds were biologically tested for their inhibitory activities against COX-2 and 5-LOX in vitro, with compound 15e showing optimal inhibitory activities. The selectivity of these compounds for COX-2 over COX-1 was also evaluated, with 15e demonstrating a selectivity index comparable to celecoxib. Additionally, the anti-inflammatory activity of selected compounds was assessed using xylene-induced ear edema in mice, albumen-induced paw edema in rats, and acetic acid-induced vascular permeability in mice models. The analgesic activity was evaluated using acetic acid-induced writhing response and hot-plate assays. Molecular modeling studies were conducted to understand the binding interactions of compound 15e with COX-2 and 5-LOX. The research suggests that compound 15e may be a promising anti-inflammatory agent for further evaluation. The reactants used in the synthesis include para-position substituted phenylhydrazine hydrochloride, ethyl 3-bromopropionate, hydroxylamine methanol solution, KOH, and various substituted phenyl rings, among others. The analyses involved high-performance liquid chromatography (HPLC), electrospray ionisation (ESI) mass spectrometry, infrared (IR) spectroscopy, and nuclear magnetic resonance (NMR) spectroscopy to determine the structures and purities of the synthesized compounds.
10.14233/ajchem.2014.16893
The research primarily focuses on the synthesis, characterization, and in vitro antitumor activity evaluation of novel Schiff base compounds containing a pyrazole group. The synthesis involved the condensation reaction of 1-arylpyrazol-4-carbaldehyde with benzene hydrazine or phenylhydrazine hydrochloride, using methanol as a solvent and refluxing at 80°C for 2 hours. The reaction was optimized to avoid the use of additional catalysts to prevent complex post-processing. The synthesized compounds were purified through crystallization using a mixture of ethanol and dichloromethane. Characterization of the compounds was achieved using nuclear magnetic resonance (NMR), infrared (IR) spectroscopy, mass spectrometry (MS), and elemental analysis. The in vitro antitumor activity was assessed by testing the compounds B2 and B4 against the K562 human leukemia cell line using the MTT assay method, with aminonide as a reference substance. The study found that these compounds exhibited antiproliferative activity against K562 cells, inhibiting their growth.
10.1016/j.bmc.2017.08.042
The research focuses on the synthesis, pharmacological activities, and molecular docking studies of pyrazolyltriazoles as potential anti-bacterial and anti-inflammatory agents. The purpose of the study was to prepare and evaluate a series of novel pyrazolyl alcohols, pyrazolyl azides, and pyrazolyltriazoles for their bioactivity profile, specifically targeting anti-bacterial and anti-inflammatory properties. The conclusions drawn from the research indicated that compound 5c exhibited potent anti-bacterial activity against Micrococcus luteus, while compounds 5f, 8b, and 8h demonstrated significant in vitro anti-inflammatory activity. Notably, compound 8h was effective in an in vivo LPS-induced sepsis model in mice, showing a significant reduction in TNF-α levels. The chemicals used in the process included various acetophenones, phenylhydrazine hydrochlorides, Vilsmeier-Haack reagents, sodium borohydride, and a range of alkynes and azides for the synthesis of the target pyrazolyltriazoles, as well as standard drugs like streptomycin and dexamethasone for comparative analysis in the biological assays.
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