Synthesis and analgesic activity of a series of new azaalkane bis-guanidinium and bis(2-aminoimidazolinium) compounds.
In the present paper, we wish to report the synthesis and antinociceptive activity of a series of new azaalkane bis(2-aminoimidazolinium) compounds from which, N,N'-di(4,5-dihydro-1H-imidazol-2-yl)-3-aza-1,6-hexanediamine 2a has shown the best analgesic properties in vivo in two different assays (i.e., acetic acid-induced writhing test and hot-plate test in mice), as well as oral bioavailability.
Dardonville
Christophe
C
Instituto de Química Médica (CSIC). Juan de la Cierva 3, 28006-, Madrid, Spain. dardonville@cf.ac.uk
Rozas
Isabel
I
Goya
Pilar
P
Girón
Rocío
R
Goicoechea
Carlos
C
Martín
Ma Isabel
MI
D019342:Acetic Acid; D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D019791:Guanidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D006168:Guinea Pigs; D006358:Hot Temperature; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008968:Molecular Conformation; D009119:Muscle Contraction / Q000187:drug effects; D018482:Muscle, Skeletal / Q000187:drug effects; D010147:Pain Measurement / Q000187:drug effects; D011930:Reaction Time / Q000187:drug effects; D013055:Spectrophotometry, Infrared
D018712:Analgesics, Non-Narcotic; D001372:Aza Compounds; D007093:Imidazoles; D007202:Indicators and Reagents; D019791:Guanidine; D019342:Acetic Acid