Montmorrilonite K10 catalyzed efficient synthesis of some 4'-nitrochalcones and their 1, 3, 5-triaryl-2-pyrazolines and in vitro antimicrobial evaluation

An expeditious synthesis of some 4´-nitrochalcones (3a-n) and their subsequent facile one-pot transformation to 1, 3,5-triaryl-2-pyrazolines (4a-n) has been carried out using montmorrilonite K10 via microwave mediated solvent free protocol.An emphasis is given to highlighting the greenness of the processes, and a fair comparison is also provided between differentinorganic solid supports as catalysts. Both conventional as well as non-conventional approaches have been explored bycomparing the reaction conditions and yields. The newly synthesized pyrazolines were studied for their in vitro antimicrobialevaluation against bacterial strains Bacillus pumilus and Escherichia coli and fungal strains Aspergillus niger and Penicilliumchrysogenum. Findings of biological evaluation highlighted 4b, 4e, 4j and 4m as potential new leads in the search of newantimicrobial agents. The structures of newly synthesized compounds have been established on the basis of elemental analysisand spectroscopic studies.Fil: Ameta, K. L.. Faculty Of Arts, Science & Commerce, Mody University Of; IndiaFil: Rathore, Nitu S.. Faculty Of Arts, Science & Commerce, Mody University Of; IndiaFil: Kumari, Maya. Faculty Of Arts, Science & Commerce, Mody University Of; IndiaFil: Khyaliya, Priyanka. University of Science and Technology; IndiaFil: Dangi R. R.. Faculty Of Arts, Science & Commerce, Mody University Of; IndiaFil: Parellada, Eduardo Alberto. Universidad Nacional de Tucumán. Facultad de Bioquímica, Química y Farmacia. Instituto de Química Orgánica. Cátedra de Química Orgánica III; Argentina. Universidad Nacional de Santiago del Estero. Instituto de Bionanotecnología del Noa. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán. Instituto de Bionanotecnología del Noa; ArgentinaFil: Neske, Adriana. Universidad Nacional de Tucumán. Facultad de Bioquímica, Química y Farmacia. Instituto de Química Orgánica. Cátedra de Química Orgánica III; Argentin

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sometamidium hydrochloride (ISMM) is an effective drug for the treatment of trypanosomosis, but it causes local and systemic toxicity. Isometamidium hydrochloride has limited therapeutic index and exhibit considerable variation in their prophylactic activities. We developed a trypanocidal nanoformulation using ISMM and polymers sodium alginate/gum acacia to enhance the efficacy of the drug at lower doses, while minimizing undesirable side effects. It was characterized by transmission electron microscopy and infrared spectroscopy for evaluation of size, morphology, functional groups, etc. In vitro cytotoxicity studies were performed by metabolic resazurin assay at different concentrations of isometamidium-loaded alginate/gum acacia nanoparticles using equine peripheral blood mononuclear cells. Hemolytic assay revealed significantly less toxicity compared to the conventional drug. The results demonstrate that …Isometamidium hydrochloride (ISMM) is an effective drug for the treatment of trypanosomosis, but it causes local and systemic toxicity. Isometamidium hydrochloride has limited therapeutic index and exhibit considerable variation in their prophylactic activities. We developed a trypanocidal nanoformulation using ISMM and polymers sodium alginate/gum acacia to enhance the efficacy of the drug at lower doses, while minimizing undesirable side effects. It was characterized by transmission electron microscopy and infrared spectroscopy for evaluation of size, morphology, functional groups, etc. In vitro cytotoxicity studies were performed by metabolic resazurin assay at different concentrations of isometamidium-loaded alginate/gum acacia nanoparticles using equine peripheral blood mononuclear cells. Hemolytic assay revealed significantly less toxicity compared to the conventional drug. The results demonstrate that the developed drug delivery module can be evaluated in suitable animal models to evaluate its potency.Not Availabl

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Not AvailableIsometamidium hydrochloride (ISMM) is an effective drug for the treatment of trypanosomosis, but it causes local and systemic toxicity. Isometamidium hydrochloride has limited therapeutic index and exhibit considerable variation in their prophylactic activities. We developed a trypanocidal nanoformulation using ISMM and polymers sodium alginate/gum acacia to enhance the efficacy of the drug at lower doses, while minimizing undesirable side effects. It was characterized by transmission electron microscopy and infrared spectroscopy for evaluation of size, morphology, functional groups, etc.In vitro cytotoxicity studies were performed by metabolic resazurin assay at different concentrations of isometamidium-loaded alginate/gum acacia nanoparticles using equine peripheral blood mononuclearcells. Hemolytic assay revealed significantly less toxicity compared to the conventional drug. The results demonstrate that the developed drug delivery module can be evaluated in suitable animal models toevaluate its potency.Not Availabl