New Quinoline-Based Compounds for Analgesic and Anti-Inflammatory Evaluation
About: This article is published in Letters in Drug Design & Discovery.The article was published on 2011-07-31. It has received 20 citations till now. The article focuses on the topics: Quinoline.
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TL;DR: The newly synthesized compounds 5a, 5c, 11b and 11c displayed excellent antimicrobial activity and their minimum inhibitory concentration (MIC) against most of test organisms was performed.
76 citations
TL;DR: Evaluation of the anticancer efficacy of quercetin loaded chitosan-quinoline nanoparticles using the in vitro cytotoxicity studies against HeLa cells indicated that the chitOSan nanoparticles are a promising candidate for the antic cancer drugs delivery.
34 citations
TL;DR: TCTA-DMF has been used as a Vilsmeier-Haack type reagent for effective synthesis of 2-chloro-3-formyl quinolines from acetanilides under conventional and ultrasonically assisted conditions.
23 citations
TL;DR: In this article, N′-((2-Chloroquinolin-3-yl)methylene)-2-cyanoacetohydrazide (3) was synthesized then treated with aromatic aldehydes in basic medium to afford the arylidene derivatives 4a-e.
Abstract: N′-((2-Chloroquinolin-3-yl)methylene)-2-cyanoacetohydrazide (3) was synthesized then treated with aromatic aldehydes in basic medium to afford the arylidene derivatives 4a–e. Reaction of 4a–c with hydrazine hydrate in boiling ethanol gave the 3-aminopyrazoles 5a–c. Base promoted Michael addition of 3 to arylidene malononitriles 6 afforded 2-pyridones 9a–d. Cyclocondensation of 3 with some salicylaldehyde derivatives gave the iminocoumarins 10a–c; these underwent acid-catalyzed hydrolysis to give coumarins 11a–c. Coupling of 3 with arene diazonium chloride in pyridine afforded the arylhydrazononitriles 12a–c. Heterocyclization of 12a with formalin and piperidine in warm ethanol gave the 1,2,4-triazine derivative 13. The mechanisms and the chemoselectively of these reactions are discussed. The newly synthesized compounds were tested for antibacterial and anticancer activity. Pyridone 9b and coumarin 11c had the most potent antibacterial activity against S. aureus. Acrylamide 4d, pyridones 9a, c, and 1,2,4-triazine 13 were the most active anticancer compounds, with a broad range of activity against most of the tumor cell lines tested.
15 citations
TL;DR: The obtained data indicated that the majority of the tested compounds exhibited antibacterial activity while all those compounds showed antifungal activity.
15 citations
References
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TL;DR: The potency ratios obtained for aspirin, phenylbutazone and hydrocortisone are fairly close to the ratios of their respective daily doses in the treatment of rheumatic disease.
Abstract: SummaryA method is presented for measuring the edema induced by injection of 0.05 ml of 1% solution of carrageenin, an extract of Chondrus, into the plantar tissues of the hind paw of the rat. Peak...
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TL;DR: 2-Acetylbenzofuran 1 on treatment with substituted aldehydes affords the corresponding chalcones 2a-c, and pyrazolines 7a-d were synthesized by treating 4a,b with phenacyl bromides in refluxing ethanol.
210 citations
TL;DR: The chemical structures of the newly synthesized compounds were characterized by IR, NMR and mass spectral analysis and screened for their analgesic and anti-inflammatory activities.
125 citations
118 citations