106729-79-7Relevant articles and documents
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists
Palin, Ronald,Abernethy, Lynn,Ansari, Nasrin,Cameron, Kenneth,Clarkson, Tom,Dempster, Maureen,Dunn, David,Easson, Anna-Marie,Edwards, Darren,MacLean, John,Everett, Katy,Feilden, Helen,Ho, Koc-Kan,Kultgen, Steve,Littlewood, Peter,McArthur, Duncan,McGregor, Deborah,McLuskey, Hazel,Neagu, Irina,Neale, Stuart,Nisbet, Lesley-Anne,Ohlmeyer, Michael,Pham, Quynhchi,Ratcliffe, Paul,Rong, Yajing,Roughton, Andrew,Sammons, Melanie,Swanson, Robert,Tracey, Heather,Walker, Glenn
, p. 892 - 898 (2011/03/21)
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Compounds 32 and 40 were found to have antihyperalgesic effects in the rat CFA Hg assay and induce a mechanism based hyperthermia.
NEW ROUTES TO CIS-1,2-HYDROXYAMINES AND RELATED SYSTEMS
Sammes, Peter G.,Thetford, Dean
, p. 2275 - 2278 (2007/10/02)
Use of modified Mitsunobu reactions followed by intramolecular cyclisations have been used to prepare cis-1,2-hydroxyamines, cis-1,3-hydroxyamines, 1,2,3-dihydroxyamines and 1,2,3-diaminoalcohols from allylic alcohols
