Refernces
10.1021/jm020335m
The study investigates a series of nonsteroidal selective glucocorticoid modulators, focusing on the effects of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. The researchers synthesized various analogues with different substituents at the C-10 position, including linear two-atom appendages such as OCH3, OCF2H, NHMe, SMe, and CH2OH, to evaluate their binding affinity for the human glucocorticoid receptor (hGR) and their anti-inflammatory effects. Key chemicals used in the study included dexamethasone and prednisolone as reference glucocorticoids, along with various synthetic intermediates and reagents like DIBAL-H for reduction reactions, trifluoromethanesulfonic anhydride for sulfonylation, and cesium carbonate for alkylation. These chemicals facilitated the preparation of the target compounds and allowed for the assessment of their biological activity in receptor binding and functional assays.
10.1016/j.steroids.2019.03.012
The study focuses on the synthesis and evaluation of novel D-ring substituted steroidal pyrazolines as potential anti-inflammatory agents. A series of steroidal derivatives with nitrogen heterocyclic side chains, specifically 4a-4l, were synthesized and tested for their anti-inflammatory effects in activated RAW 264.7 macrophage cells. The synthesis process involved two steps: Claisen-Schmidt condensation with pregnenolone and aromatic aldehydes, followed by nucleophilic addition of thiosemicarbazide to an α, β-unsaturated carbonyl. The synthesized compounds were confirmed by 1H-NMR, 13C-NMR, HRMS, and IR analyses. The purpose of these chemicals was to identify new potential anti-inflammatory agents that could be considered for further research and development in designing anti-inflammatory drugs. Among the synthesized compounds, 4g showed the most potent anti-inflammatory activity with an IC50 value of 0.86 μM on nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 cells, comparable to dexamethasone, and low cytotoxicity, making it a promising therapeutic anti-inflammatory drug candidate.
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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