Search results for "COX inhibitors"

showing 2 items of 2 documents

Synthesis and COX inhibition of 7-R1-8-R2-1-ethyl-3,4-dimethyl-, 4,10-dihydro-1H-pyrazolo[3,4-c][1,5]benzodiazocine-5,11-diones

2008

The title compounds were easily synthesized by reacting the 4-aminopyrazole hydrochloride 2 and the substituted 2-nitrobenzoyl chlorides 3a-d. The obtained 2-nitrobenzamides 4a-d were methylated and then reduced to give the corresponding amines 6a-d. These were hydrolyzed then directly converted into 4,10-dihydro-1H-pyrazolo[3,4-c][1,5]benzodiazocine-5,11-diones 1a-d by the action of SOCl2 in benzene. These were tested for their COX inhibitory activity, showing an inhibitory profile against both COX-1 and COX-2, being slightly more selective against COX-2 with a percentage of inhibition, at the concentration of 10 μM, in the range 42.0 – 55.0.

Hydrolysischemistry.chemical_compoundchemistryHydrochlorideOrganic ChemistryPyrazoleCOX inhibitorsPyrazolePyrazole; COX inhibitorsBenzeneSettore CHIM/08 - Chimica FarmaceuticaMedicinal chemistryPyrazole COX inhibitors
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Synthesis of pyrazolo[4,3-c][1,2,6]benzothiadiazocine, a new ring system as potential COX inhibitor

2012

Derivatives of the new ring system 1,4-dihydropyrazolo[4,3-c][1,2,6] benzothiadiazocin-11(10H)one 5,5-dioxide were synthesized in five or six steps in 57-66% overall yields and tested as COX inhibitors.

lcsh:QD241-441chemistry.chemical_compoundCOX Inhibitorlcsh:Organic chemistryChemistryStereochemistry[126]Benzothiadiazocine 14-dihydropyrazolo[43-c][126benzothiadiazocin-11(10H)one 55-dioxides pyrazole COX inhibitorsOrganic ChemistryPyrazoleRing (chemistry)Settore CHIM/08 - Chimica FarmaceuticaARKIVOC
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