144252-14-2Relevant academic research and scientific papers
TRPA1 MODULATORS
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Paragraph 0206-0207, (2015/07/16)
This disclosure relates to polycyclic heteroaromatic compounds useful as TRPA1 modulators, as well as compositions and methods of treating pain that include the compounds.
Design, synthesis and biological screening of some pyridinylpyrazole and pyridinylisoxazole derivatives as potential anti-inflammatory, analgesic, antipyretic and antimicrobial agents
El-Hawash, Soad A.M.,Soliman, Raafat,Youssef, Amal M.,Ragab, Hanan M.A.,Elzahhar, Perihan A.S.,El-Ashmawey, Ibrahim M.,Wahab, Abeer E. Abdel,Shaat, Iman A.
, p. 318 - 338 (2014/05/06)
A series of substituted pyridinylpyrazole (or isoxazole) derivatives was synthesized and evaluated for their antiinflammatory (AI) activity using formalin-induced paw edema bioassays. The inhibitory activities of cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2) were also determined. The analgesic activity of the same compounds was evaluated using rat-tail withdrawal technique. Their antipyretic activity was also evaluated. The results revealed that compounds 4a,b, 6a, 8a, 14c and 15a exhibited significant AI and analgesic activities. Compounds 5a, 6a and 8a displayed good antipyretic activity. Compounds 14c and 15a showed good COX-2 inhibitory activity and weak inhibition of COX- 1. Additionally, the most active compounds were shown to have a large safety margin (ALD50 >300-400 mg/Kg) and minimal ulcerogenic potentialities when administered orally at a dose of 300 mg/Kg. Docking studies for 14c and 15a with COX-2 showed good binding profile. Antimicrobial evaluation proved that most of the compounds exhibited distinctive activity against the gram negative bacteria, P. aeruginosa and E coli.
