Khan, Abida published the artcileDiscovery of novel pyridazine-based cyclooxygenase-2 inhibitors with a promising gastric safety profile, COA of Formula: C10H10O3, the publication is Molecules (2020), 25(9), 2002, database is CAplus and MEDLINE.
Cyclooxygenase-2 (COX-2) is implicated in the development of chronic inflammatory diseases. Recently, pyridazine derivatives have emerged as a novel prototype to develop COX-2 inhibitors. Herein, some pyridazine-based COX-2 inhibitors I [R = H2N, H2NC(S)NH, (4-oxo-4,5-dihydro-1,3-thiazol-2-yl)amino, (4-phenyl-1,3-thiazol-2-yl)amino, (5-[(dimethylamino)methylidene]-4-oxo-4,5-dihydro-1,3-thiazol-2-yl)amino, etc.] were synthesized and assessed for COX-1 and COX-2 inhibitory action, gastric ulcerogenic effects, and lipid peroxidation properties. Mol. docking studies and determination of the physicochem. parameters were also carried out. The compounds I [R = (4-phenyl-1,3-thiazol-2-yl)amino] (IC50 = 15.50 nM, 114.77%), I [R = (4-(4-bromophenyl)-1,3-thiazol-2-yl)amino] (IC50 = 17.50 nM, 101.65%), I [R = (4-oxo-5-(2-oxo-2,3-dihydro-1H-indol-3-ylidene)-4,5-dihydro-1,3-thiazol-2-yl)amino] (IC50 = 17.10 nM, 104.03%), I [R = ((5Z)-5-[(4-methoxyphenyl)methylidene]-4-oxo-4,5-dihydro-1,3-thiazol-2-yl)amino] (IC50 = 16.90 nM, 105.26%), and I [R = (4-oxo-3-phenyl-1,3-thiazol-2-ylidene)imino] (IC50 = 17.70 nM, 100.5%) displayed better COX-2 inhibition than celecoxib (IC50 = 17.79 nM, 100%). These outcomes were harmonious with the mol. docking studies of these 5 compounds These compounds also displayed comparable onset and the duration of action concerning celecoxib and indomethacin in the in vivo studies. No ulcerogenic effects were observed for I [R = (4-phenyl-1,3-thiazol-2-yl)amino, (4-oxo-5-(2-oxo-2,3-dihydro-1H-indol-3-ylidene)-4,5-dihydro-1,3-thiazol-2-yl)amino], whereas I [R = (4-(4-bromophenyl)-1,3-thiazol-2-yl)amino, ((5Z)-5-[(4-methoxyphenyl)methylidene]-4-oxo-4,5-dihydro-1,3-thiazol-2-yl)amino, (4-oxo-3-phenyl-1,3-thiazol-2-ylidene)imino] showed an insignificant ulcerogenic effect compared to celecoxib. These 5 compounds displayed a better lipid peroxidation profile than celecoxib and indomethacin and appreciable calculated absorption compared to celecoxib, and have been recognized and postulated as non-ulcerogenic COX-2 inhibitors with promising physicochem. parameters and gastric safety profile. These compounds may be useful candidates to combat diseases caused by higher levels of COX-2.
Molecules published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, COA of Formula: C10H10O3.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia