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1.
Yakugaku Zasshi ; 136(9): 1233-42, 2016 09 01.
Artículo en Japonés | MEDLINE | ID: mdl-27301389

RESUMEN

Environmental cleaning and disinfection plays an important role as a part of the standard precautions to prevent healthcare-associated infections, whereas hand hygiene is one of the most important strategies for breaking the chain of transmission. Cleaning and disinfection of high-touch areas in a health-care facility is emphasized. And wiping with an alcohol-saturated cloth which has features such as low corrosion and a wide range of antimicrobial activity is performed commonly for this purpose. Although alcohol provides immediate activity against enveloped viruses, its virucidal activity against certain non-enveloped viruses, including norovirus, is insufficient. We created a novel alcohol-based hand rub, MR06B7, which is safe for the skin, and is active against an extended spectrum of microorganisms including non-enveloped viruses. For environmental surface disinfection, a novel disinfectant MR13B15, which is based on MR06B7, has been developed. In vitro antimicrobial activity against a variety of pathogens, material compatibility, and simulated surface disinfection and decontamination efficacy of MR13B15 were investigated. According to the results, MR13B15 demonstrated potent bactericidal, fungicidal, mycobactericidal, and virucidal activity within a short contact time in addition to superior efficacy against non-enveloped viruses compared to ethanol for disinfection. Moreover, MR13B15 showed better material compatibility. Two simulation tests conducted for evaluating the disinfection and decontamination potency on environmental surfaces against feline calicivirus, a surrogate for norovirus, indicated that MR13B15 had superior efficacy for surface treatment compared to ethanol. These findings suggest that MR13B15, which satisfies most requirements of an environmental surface disinfectant, may contribute to accomplishing advanced standard precautions in preventing infections.


Asunto(s)
Antiinfecciosos , Detergentes/química , Desinfectantes/química , Instituciones de Salud , Control de Infecciones , Alcoholes , Detergentes/síntesis química , Detergentes/farmacología , Desinfectantes/síntesis química , Desinfectantes/farmacología
2.
Chem Pharm Bull (Tokyo) ; 55(12): 1682-8, 2007 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-18057740

RESUMEN

We developed new intravenous sedative-hypnotic compounds with the isoindolin-1-one skeleton focusing on the water-soluble property and in vivo safety. We synthesized approximately 170 derivatives and evaluated their hypnotic effects by intravenous administration of the compounds to mice. A series of the 2-phenyl-3-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]isoindolin-1-one analogs, 3(-), 5(-), 27(-), and 47(-) [JM-1232(-)], showed potent sedative-hypnotic activity with good water solubility and a wide safety margin. The hypnotic doses (HD50s) of these 4 compounds when administered to mice were 2.35, 1.90, 2.17, and 3.12 mg/kg, respectively, and the lethal doses (LD50s) were 88.67, 64.69, >120, and >120 mg/kg, respectively. The therapeutic indexes (LD50/HD50) were 37.73, 34.05, >55.30, and >38.46, respectively. Among these compound, 47(-) [JM-1232(-)] is being considered as the most potential candidate for clinical trials in humans.


Asunto(s)
Hipnóticos y Sedantes , Isoindoles/farmacología , Animales , Fenómenos Químicos , Química Física , Inyecciones Intravenosas , Isoindoles/síntesis química , Isoindoles/toxicidad , Dosificación Letal Mediana , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Ratones Endogámicos ICR , Sueño/efectos de los fármacos , Solubilidad , Estereoisomerismo
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