A specific and direct comparison of the trifluoromethyl and pentafluoro sulfanyl groups on the selective dopamine D(3) antagonist 3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0]hexane template.
A direct and specific comparison of a trifluoromethyl group with the corresponding pentafluorosulfanyl group is made in terms of primary affinity and pharmacokinetic properties.
Micheli
Fabrizio
F
Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Verona, Italy. fm20244@gsk.com
Andreotti
Daniele
D
Braggio
Simone
S
Checchia
Anna
A
D000818:Animals; D053961:Azabicyclo Compounds / Q000737:chemistry* / Q000493:pharmacokinetics; D005461:Fluorine / Q000737:chemistry*; D006574:Heterocyclic Compounds, 2-Ring / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013455:Sulfur / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry* / Q000493:pharmacokinetics
C553353:3-(3-((4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl)thio)propyl)-1-phenyl-3-azabicyclo(3.1.0)hexane; D053961:Azabicyclo Compounds; D006574:Heterocyclic Compounds, 2-Ring; D050637:Receptors, Dopamine D3; D014230:Triazoles; D005461:Fluorine; D013455:Sulfur