Chemical Research Letters, May 2021. As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world., SDS of cas: 57-71-6, Introducing a new discovery about 57-71-6, Name is Diacetyl Monoxime, molecular formula is C4H7NO2, belongs to pyrrolines compound. In a document, author is Shen, F.
Inhibitory effect of 3,4-diaryl-3-pyrrolin-2-one derivatives on cyclooxygenase 1 and 2 in murine peritoneal macrophages
AIM: To develop a whole-cell assay based on murine peritoneal macrophages and evaluate the inhibitory effect of candidate compounds on cyclooxygenase-1 (COX-1) and COX-2. METHODS: Macrophages were stimulated with calcimycin or hpopolysaccharide (LPS) for various periods. Their abilities to convert endogenous arachidonic acid to 6-keto-PGF(1alpha) or PGE(2) were examined by radioimmunoassay (RIA). RNA level of glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and COX-1/2 was detected by reverse transcription polymerase chain reaction (RT-PCR) using specific primers. RESULTS: Rofecoxib selectively inhibited LPS-induced, COX-2-derived PGE(2) synthesis with an IC50 value of (4.7+/-0.5) nmol/L compared with maximum inhibitory ratio of 17.3 % for the inhibition of calcimycin induced, COX-1-derived 6-keto-PGF(1alpha) synthesis. Indomethacin exhibited dual inhibitory effects on COX-1 and COX-2 with IC50 of (4.7+/-1.1) nmol/L and (7.1+/-1.2) nmol/L, respectively. Two series of 17 compounds were tested. Most of compounds in series 11 showed comparable inhibitory activities to rofecoxib on COX-2. The relative position of the sulfonylphenyl group to the lactam carbonyl group has important effects on COX-2 inhibitory activity. CONCLUSION: The established whole cell assay is appropriate for drug-design oriented in vitro assay. 3,4-Diaryl-3-pyrrolin-2-one derivatives were proved to be prospective new type of COX-2 selective inhibitors.
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Reference:
Pyrroline – Wikipedia,
,1-Pyrroline | C4H7N – PubChem