Synthesis by microwave irradiation and antidiarrhoeal activity of benzotriazinone and saccharine derivatives.
The synthesis by microwave irradiation and the biological results of novel benzotriazinone and saccharine derivatives with potential antidiarrhoeal activity is described. Conventional and microwave heatings were compared for the reactions. Good yields and short reaction times are the main advantages of our synthetic route. Among the tested compounds, compound 12 inhibited motility both in in-vitro and in-vivo tests.
Fiorino
Ferdinando
F
Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli, "Federico II", Napoli, Italy.
Caliendo
Giuseppe
G
Perissutti
Elisa
E
Severino
Beatrice
B
Frecentese
Francesco
F
Preziosi
Barbara
B
Izzo
Angelo A
AA
Capasso
Raffaele
R
Santagada
Vincenzo
V
D000818:Animals; D000930:Antidiarrheals / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D004558:Electric Stimulation; D005772:Gastrointestinal Transit / Q000187:drug effects*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D051379:Mice; D008813:Mice, Inbred ICR; D008872:Microwaves; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D012439:Saccharin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000930:Antidiarrheals; D014227:Triazines; D012439:Saccharin