Anti-inflammatory, analgesic and antipyretic 4,6-disubstituted 3-cyanopyridine-2-ones and 3-cyano-2-aminopyridines

Manna, Fedele; Chimenti, Franco; Bolasco, Adriana; Filippelli, Amelia; Palla, A.; Filippelli, Walter; Lampa, E; Mercantini, R.

doi:10.1016/0223-5234(92)90141-m

Cited by 57 publications

(26 citation statements)

References 6 publications

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“…All compounds synthesized were also tested for urease inhibitory activities. From the chalcones, only 22 was found to be active (IC 50 32.51 mm ; Table 3). However, a number of benzothiazepines showed very promising activitites, with IC 50 values as low as 19 mm (33).…”

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confidence: 97%

Syntheses and Biological Activities of Chalcone and 1,5-Benzothiazepine Derivatives: Promising New Free-Radical Scavengers, and Esterase, Urease, and?-Glucosidase Inhibitors

Ansari

Umbreen

Hussain

et al. 2005

C&B

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A series of 2,4-diaryl-2,3,4,5-tetrahydro- (36-40) and 2,4-diaryl-2,3-dihydro-1,5-benzothiazepines (25-35) have been synthesized from the corresponding chalcones 1-24. Both the benzothiazepines and chalcones were evaluated as DPPH free-radical scavengers and as inhibitors of cholinesterases, urease, and alpha-glucosidase. Compounds 2, 5, 6, 7, 10, 13, 18, 21, 36a, 37a, 37b, and 39a showed significant cholinesterase inhibiting activities. Among the 15 dihydro-1,5-benzothiazepines, 26, 32, and 35 exhibited significant radical-scavenging activities; and six tetrahydro-1,5-benzothiazepines (35, 36a, 36b, 37a, 37b, and 39a) were found to be inhibitors of AChE and BChE. Compounds 22, 25, 26, 33, 35, 36a, 37b, and 39a inhibited urease, and 25 and 27-31 were found to be potent inhibitors of alpha-glucosidase.

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confidence: 97%

Syntheses and Biological Activities of Chalcone and 1,5-Benzothiazepine Derivatives: Promising New Free-Radical Scavengers, and Esterase, Urease, and?-Glucosidase Inhibitors

Ansari

Umbreen

Hussain

et al. 2005

C&B

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“…The 4-substitution of antipyrine and derivatives of 4-aminoantipyrine proved to be more active than the parent compounds [1]. On the other hand, 3-cyano-4,6-diarylpyridin-2-ones exhibited marked anti-inflammatory and/or analgesic activities [2]. Furthermore, many fused pyridine derivatives such as pyrazolo [3,4-b]pyridines induced reduction of pro-inflammatory cytokines and were found to possess anti-inflammatory and analgesic activities [3,4].…”

Section: Introductionmentioning

confidence: 93%

“…The administered oral dose of the tested compound (50 mg/kg body weight) was calculated according to the literature [2] and the negative control group received 1 mL of water suspended in tween 80.…”

Section: Preparation Of Samplesmentioning

confidence: 99%

Synthesis of Novel 1‐Pyrazolylpyridin‐2‐ones as Potential Anti‐Inflammatory and Analgesic Agents

Ismail

Ammar

El‐Zahaby

et al. 2007

Archiv der Pharmazie

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A new series of 4-alkyl/aryl-2-oxo-1-pyrazolyl-1,2-dihydropyridine-3-carbonitriles, pyrazolo[3,4-b]pyridine-5-carbonitriles and pyrido[2,3-d]pyrimidine-6-carbonitriles have been synthesized and tested for their anti-inflammatory and analgesic activities. Among the tested compounds, 3e and 8b exhibited comparable anti-inflammatory activity to the standard (indomethacin). Compounds 5, 7a, and 8b displayed potent analgesic activity. Detailed syntheses, spectroscopic and biological data are reported.

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“…The pyridine dicarbonitrile substructure was therefore chosen as a basic structural scaffold for the design of a reaction-based library (Reddy et al, 2006). Many publications report the biological properties of pyridinedicarbonitriles as being antihypertensive (Ward, 1976), antihistaminic (Quintela et al, 1997), anticancer, (Cocco et al, 2007) anti-inflammatory, analgesic (Manna et al, 1992), antibacterial (Behbehani et al, 2012), anti-HIV agents (El-Hawash et al, 2006) and anti-Alzheimer (Samadi et al, 2010). Many derivatives of pyridine-3,5-dicarbonitrile are reported as potential therapeutic agents, In hope to discover novel therapeutic agents, a series of 6-amino-1-(5, 6-dimethoxy-2,3-dihydro-1H-inden-1-ylideneamino)-2-oxo-4-aryl-1,2-dihydropyridine-3,5-dicarbonitrile compound are prepared which have not been reported before and compounds are tested for their antibacterial and antifungal activities.…”

Section: Introductionmentioning

confidence: 99%

Novel derivatives of 5,6-dimethoxy-1-indanone coupled with substituted pyridine as potential antimicrobial agents

Patel

Bhatt

et al. 2018

Arabian Journal of Chemistry

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Synthesis of novel derivatives of 5,6-dimethoxy-1-indanone was carried out via its Schiff's base using 2-cyanoacetohydrazide followed by cyclization with 2-arylidenemalononitrile in the presence of a catalytical amount of piperidine to get 6-amino-1-(5,6-dimethoxy-2,3-dihydro-1H-inden-1-ylideneamino)-2-oxo-4-aryl-1,2-dihydropyridine-3,5-dicarbonitrile derivatives. The structures of the synthesized compounds were confirmed on the basis of their spectral and elemental analysis. The synthesized compounds were also screened for antimicrobial activity and found to have promising antibacterial activity.

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Anti-inflammatory, analgesic and antipyretic 4,6-disubstituted 3-cyanopyridine-2-ones and 3-cyano-2-aminopyridines

Cited by 57 publications

References 6 publications

Syntheses and Biological Activities of Chalcone and 1,5-Benzothiazepine Derivatives: Promising New Free-Radical Scavengers, and Esterase, Urease, and?-Glucosidase Inhibitors

Syntheses and Biological Activities of Chalcone and 1,5-Benzothiazepine Derivatives: Promising New Free-Radical Scavengers, and Esterase, Urease, and?-Glucosidase Inhibitors

Synthesis of Novel 1‐Pyrazolylpyridin‐2‐ones as Potential Anti‐Inflammatory and Analgesic Agents

Novel derivatives of 5,6-dimethoxy-1-indanone coupled with substituted pyridine as potential antimicrobial agents

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