Bhandari, Shashikant V. published the artcileDesign, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs, Name: 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is diarylpyrazolinone preparation; ethyl acetoacetate diethylmalonate benzoyl chloride condensation cyclocondensation nucleophilic substitution; NSAID inflammation antiinflammatory pain analgesic structure activity vasorelaxant; prostaglandin synthase COX2 inhibitor mol simulation acute ulcerogenicity histopathol.
Various substituted 1,5-diarylpyrazol-3-one derivatives were synthesized and screened for analgesic, anti-inflammatory activities, ulcerogenic potential and for their ability to release nitric oxide. Most compounds exhibited significant analgesic and anti-inflammatory activities. It was interesting to note that out of ten compounds, I (R = H) (59.64%) was found to have anti-inflammatory activity greater than the standard drug Indomethacin (57.89%), whereas II (R = 2-OMe) (57.89%) was found to be equipotent to that of standard, Indomethacin. The pharmacol. studies suggested that the presence of 4-nitro and 2-methoxy on Ph ring at C5 of pyrazole has a significant anti-inflammatory activity and 4-chloro substitution on same Ph ring was found to have decreased activity. However only a Ph substituted derivative was found to have most potent activity. I (R = H) containing plane Ph at C5 of pyrazole was found to have significant analgesic activity (56.86%) in acetic acid induced writhing model. I and II (R = 4-Cl) having 4-chloro substituted Ph ring showed least analgesic activity (10.78%) and (6.86%) resp. The compounds also showed significantly reduced GI-ulcerogenicity and gastroprotective results in histopathol. studies i.e. they were found to be causing no mucosal injury. All the synthesized compounds were found to exhibit significant nitric oxide releasing activity, in both in vitro and in vivo models. Mol. docking studies served to be an important tool for the study of binding of compounds with that of a COX-2 enzyme. The results of the docking studies were found to endorse the result of exptl. work. Thus, the rationale used to design the NCEs was found to produce the promising results as anticipated. Therefore it can be said that the strategy employed can serve as an important tool in future for the design and development of novel therapeutic agents of various categories too.
European Journal of Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Name: 5-Phenyl-1H-pyrazol-3(2H)-one.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics