Zobrazeno 1 - 2
of 2
pro vyhledávání: '"Steve Kultgen"'
Autor:
Lynn Abernethy, Quynhchi Pham, Helen Feilden, Olaf Nimz, Yajing Rong, Michael Ohlmeyer, Anna-Marie Easson, David A. Dunn, Heather Tracey, Littlewood Peter Thomas Albert, Steve Kultgen, Lesley-Anne Nisbet, John Maclean, Maureen Dempster, Duncan McArthur, Robert Swanson, Melanie Sammons, Ronnie Palin, Andrew Laird Roughton, Darren Edwards, Kenneth S. Cameron, Deborah McGregor, Paul Ratcliffe, Irina Neagu, Hazel McLuskey, Koc-Kan Ho, Katy Everett, Thomas R. Clarkson, Glenn Walker, Nasrin Ansari
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(15)
Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted. Substitution of the 4-position with specific polar functionality afforded the requisite balance of potency, solubility and physicochemical properties.
Autor:
Michael Ohlmeyer, Yajing Rong, Katy Everett, Robert Swanson, Nasrin Ansari, Duncan McArthur, Kenneth S. Cameron, Quynhchi Pham, Irina Neagu, Heather Tracey, Darren Edwards, John Maclean, Maureen Dempster, Thomas R. Clarkson, Hazel McLuskey, Koc-Kan Ho, Helen Feilden, Paul Ratcliffe, David A. Dunn, Andrew Laird Roughton, S.A. Neale, Steve Kultgen, Glenn Walker, Littlewood Peter Thomas Albert, Melanie Sammons, Ronald Palin, Lynn Abernethy, Anna-Marie Easson, Deborah McGregor, Lesley-Anne Nisbet
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(3)
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. Co