Synthesis and biological evaluation of 2,3-diarylthiophenes as selective Cox-2 and Cox-1 inhibitors
Several 2,3-diarythiophene compounds were prepared and their activities against both cyclooxygenase isoforms were evaluated.
References (17)
- et al.
J. Biol. Chem.
(1993) - et al.
J. Biol. Chem.
(1992) - et al.
Bioorg. Med. Chem. Lett.
(1995) - et al.
Arch. Biochem. Biophys.
(1994) Nature [New Biol.]
(1971)- et al.
Nature [New Biol.]
(1971) - et al.
- et al.
Mol. Pharmacol.
(1994)
Cited by (67)
Dithiane-Induced [3+2] Cycloaddition Tactic for the Convergent Synthesis of Dihydropyrrole and Pyrrole Derivatives
2020, Journal of Organic ChemistryMedicinal chemistry of vicinal diaryl scaffold: A mini review
2019, European Journal of Medicinal ChemistryCitation Excerpt :Similarly, Pal et al. [21] reported 1,5-diarylpyrazole 22 as a sodium salt of benzenesulfonamide for injectables (Fig. 4). Merck researchers exploited Dup 697 (1) to understand the biological activity, selectivity and structure activity relationship (SAR) around the thiophene, a central ring, was explored in search of new COX-2 inhibitors [22]. Later, they replaced the central ring thiophene by various hetreocycles like thiazole, isothiazole, thiadiazole, imidazole, triazole and tetrazole.
Chemical and Biological Profiles of Vicinal Diaryl-substituted Thiophenes, Imidazolines, Selendiazoles, and Isoselenazoles
2018, Vicinal Diaryl Substituted Heterocycles: A Gold Mine for the Discovery of Novel Therapeutic AgentsSynthesis and Biological Activities of Vicinal Diaryl Furans
2018, Vicinal Diaryl Substituted Heterocycles: A Gold Mine for the Discovery of Novel Therapeutic AgentsDiscovery of potential and selective COX-1 inhibitory leads using pharmacophore modelling, in silico screening and in vitro evaluation
2014, European Journal of Medicinal ChemistryCitation Excerpt :These compounds displayed poor selectivity towards COX-2 which may be due to the absence of methylsulfonyl or sulfamoyl groups. Other structure–activity relationship studies have confirmed that the presence of a 4-methylsulfonyl or 4-sulfamoyl group on the phenyl ring of the inhibitor provides COX-2 selectivity and that no other substitution is tolerated [40,41]. The other factor which seems necessary for COX-2 selectivity is the difference in the size and shape of the active site of COX-2 to that of COX-1.
Synthesis and biological activity evaluation of lignan lactones derived from (-)-cubebin
2005, Bioorganic and Medicinal Chemistry Letters