Assuntos
Antivirais/uso terapêutico , Indóis/uso terapêutico , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Influenza Humana/tratamento farmacológico , Oseltamivir/uso terapêutico , Extratos Vegetais/uso terapêutico , Zanamivir/uso terapêutico , Antivirais/efeitos adversos , Combinação de Medicamentos , Sinergismo Farmacológico , Humanos , Indóis/efeitos adversos , Vírus da Influenza A Subtipo H1N1/patogenicidade , Influenza Humana/diagnóstico , Influenza Humana/virologia , Oseltamivir/efeitos adversos , Extratos Vegetais/efeitos adversos , Resultado do Tratamento , Zanamivir/efeitos adversosRESUMO
Dimethylallylguanidine, also known as galegine, isolated from Galega officinalis, has been shown to have weight reducing properties in vivo. Substitution of the guanidine group with an N-cyano group and replacement of guanidine with amidine, pyrimidine, pyridine, or the imidazole moieties removed the weight reducing properties when evaluated in BALB/c mice. However, retention of the guanidine and replacement of the dimethylallyl group by a series of functionalized benzyl substituents was shown to exhibit, and in some cases significantly improve, the weight reducing properties of these molecules in BALB/c, ob/ob, and diet induced obesity (DIO) mice models. The lead compound identified, across all models, was 1-(4-chlorobenzyl)guanidine hemisulfate, which gave an average daily weight difference (% from time-matched controls; +/- SEM) of -19.7 +/- 1.0, -11.0 +/- 0.7, and -7.3 +/- 0.8 in BALB/c, ob/ob, and DIO models, respectively.
