Abstract
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.
MeSH terms
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Animals
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Antidiarrheals / chemical synthesis*
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Antidiarrheals / chemistry
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Antidiarrheals / pharmacology
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Chemistry, Pharmaceutical
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Electric Stimulation
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Gastrointestinal Transit / drug effects*
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Guinea Pigs
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Ileum / drug effects
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In Vitro Techniques
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Mice
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Mice, Inbred ICR
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Microwaves*
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Molecular Structure
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Saccharin / analogs & derivatives*
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Saccharin / chemical synthesis*
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Saccharin / pharmacology
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Structure-Activity Relationship
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Triazines / chemical synthesis*
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Triazines / chemistry
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Triazines / pharmacology
Substances
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Antidiarrheals
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Triazines
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Saccharin