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Densely Functionalized 2-Methylideneazetidines: Evaluation as Antibacterials.
Molecules
June 2021
Department of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via E. Orabona n. 4, 70126 Bari, Italy.
Twenty-two novel, variously substituted nitroazetidines were designed as both sulfonamide and urethane vinylogs possibly endowed with antimicrobial activity. The compounds under study were obtained following a general procedure recently developed, starting from 4-nitropentadienoates deriving from a common β-nitrothiophenic precursor. While being devoid of any activity against fungi and Gram-negative bacteria, most of the title compounds performed as potent antibacterial agents on Gram-positive bacteria ( and three strains of ), with the most potent congener being the 1-(4-chlorobenzyl)-3-nitro-4-(-tolyl)azetidine , which displayed potency close to that of norfloxacin, the reference antibiotic (minimum inhibitory concentration values 4 and 1-2 μg/mL, respectively).
View Article and Find Full Text PDFToxico-pharmacological evaluations of the small-molecule LQFM166: Inducer of apoptosis and MDM2 antagonist.
Chem Biol Interact
September 2018
Laboratory of Cellular Pharmacology and Toxicology, Faculty of Pharmacy, Federal University of Goiás, Goiânia, Goiás, Brazil. Electronic address:
Inhibition of p53-MDM2 complex has been emerging as a strategy for antitumoral drug development considering the pro-apoptotic role of functional p53 in tumor cells. In our study, the prototype LQFM166 (2), designed through molecular simplification strategy inspired in the Nutlins compounds, was synthetized, characterized and the mechanisms of cell death were investigated. In addition, we estimated the starting doses for acute oral systemic toxicity tests according to the OECD Guidance Document No.
View Article and Find Full Text PDFPaths to the discovery of antivenom serotherapy in France.
J Venom Anim Toxins Incl Trop Dis
June 2016
Laboratory for Scientific and Technological Information on Health (LICTS), Institute for Communication and Scientific and Technological Information on Health (ICICT), Oswaldo Cruz Foundation (FIOCRUZ), Av. Brasil, 4365 - Prédio Haity Moussatché, 2° andar, sala 206, 21045-360 Rio de Janeiro, RJ Brazil ; National Toxico-Pharmacological Information System (SINITOX), Av. Brasil, 4365 - Prédio Haity Moussatché, 2° andar, sala 206, 21045-360 Rio de Janeiro, RJ Brazil ; Post-Graduate Program in Health Information and Communication (PPGICS), ICICT, Av. Brasil, 4365 - Prédio Haity Moussatché, 2° andar, sala 206, 21045-360 Rio de Janeiro, RJ Brazil.
The current study presents a descriptive chronological survey of the articles published by Césaire Auguste Phisalix and Albert Calmette on snake poison, with the aim of shedding a light on the areas of research and reasoning followed by these scientists, leading up to their simultaneous discovery of antivenom serotherapy in 1894. The path taken by Phisalix is revealed in 15 articles that demonstrate the motivation of a naturalist and the way he confronted the puzzle of immunity against snake venom. In the case of Calmette, two articles preceded the discovery; microbiology was his theoretical base and the Pasteurian spirit of solving health problems his driving force.
View Article and Find Full Text PDFUse of L. (Asteraceae) and L. (Zingiberaceae) to treat intestinal mucositis in mice: Toxico-pharmacological evaluations.
Toxicol Rep
October 2015
Laboratório de Farmacologia e Toxicologia Celular-FarmaTec, Faculdade de Farmácia, Universidade Federal de Goiás (UFG), Goiânia, GO, Brazil.
Introduction: Several studies towards the development of an effective treatment for intestinal mucositis have been reported, since this condition represents a major problem in clinical oncology practice due to cytotoxic effects of chemotherapy. However standardized protocols and universally accepted treatment options are yet to be established.
Objectives: Given above, this study evaluated the protective effects of a mucoadhesive formulation containing both L.
Flatworm models in pharmacological research: the importance of compound stability testing.
Regul Toxicol Pharmacol
October 2014
Drug Quality and Registration (DruQuaR) Group, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460 (Second Floor), 9000 Ghent, Belgium. Electronic address:
Flatworms possess adult pluripotent stem cells, which make them extraordinary experimental model organisms to assess in vivo the undesirable effects of substances on stem cells. Currently, quality practices, implying evaluation of the stability of the test compound under the proposed experimental conditions, are uncommon in this research field. Nevertheless, performing a stability study during the rational design of in vivo assay protocols will result in more reliable assay results.
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