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Synthesis, Cyclooxygenase Inhibition, Anti-Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5-Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore

, : Synthesis, Cyclooxygenase Inhibition, Anti-Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5-Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore. Archiv der Pharmazie 349(10): 801-807

NlmCategory="UNASSIGNED">A new series of 1,3,5-triarylpyrazolines 13a-l was synthesized and all prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and in vivo anti-inflammatory activity. All test compounds were more selective for the COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 13h was the most COX-2 selective compound (COX-2 selectivity index (SI) = 10.23) and the most potent anti-inflammatory derivative (ED50  = 60.1 µmol/kg) in comparison with celecoxib (COX-2 SI = 9.29 and ED50  = 81.4 µmol/kg). All screened compounds were less ulcerogenic (ulcer indexes (UI) = 0.33-1.33) than aspirin (UI = 2.33) and comparable to celecoxib (UI = 0.33).


PMID: 27601359

DOI: 10.1002/ardp.201600145

Other references

Markowitz, J.C., 1997: Dysthymic disorder in the context of other psychiatric disorders. American Family Physician 55(5): 1579-800, 1583

J.A.G.ant; R.E.A.vidson; L.S.C.umpler; M.P.G.lombek;; A.F.C.H.ldemann; R.L.; L.A.S.derblom; S.W.S.uyres; S.P.W.ight; W.A.W.tters, 2006: Crater gradation in Gusev Crater and Meridiani Planum, Mars. Journal of Geophysical Research: Planets 111(E2)

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Lepage, V.; Gluckman, J.C.; Bedrossian, J.; Duboust, A.; Nebout, T.; Bracq, C.; Rudloff, M.C.; Dausset, J., 1978: Anti-B cell lymphocytotoxic antibodies in kidney transplant recipients. Serial serum samples from 47 renal allotransplant recipients were screened for antiperipheral blood lymphocyte, anti-B cell, and anti-Daudi cell line antibodies. Various associations of these antibodies were observed in 28 patients. Anti-Daudi did...

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Rabovich, R.D.; Poznanskii, S.S., 1954: Typical plan for practical training in the field of hygiene in therapeutic and pediatric departments of medical institutes. Gigiena i Sanitariia 9: 41-45