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141.
Valentina Ferrari Michaela Serpi Christopher McGuigan 《Nucleosides, nucleotides & nucleic acids》2015,34(11):799-814
Protection and deprotection strategies involving the N-acetyl group are widely utilized in nucleoside and nucleotide chemistry. Herein, we present a mild and selective N-deacetylation methodology, applicable to purine and pyrimidine nucleosides, by means of Schwartz's reagent, compatible with most of the common protecting groups used in nucleoside chemistry. 相似文献
142.
143.
Graziella Hanna Pereira Aline Queiroz Santos Miriam Park Patricia Rady Muller Soraia Padua Raquel Ferrari Marchesi Vera Lucia Aldred 《Mycopathologia》2010,170(4):259-261
Paracoccidioides brasiliensis rarely shows bone marrow involvement and its response to treatment with itraconazole in children needs further assessment. We describe here a child with a juvenile disseminated form of paracoccidioidomycosis, which showed reticuloendothelial system involvement and the presence of Paracoccidioides brasiliensis in the bone marrow. The patient showed an effective and rapid response to itraconazole therapy. 相似文献
144.
Cappelli A Valenti S Mancini A Giuliani G Anzini M Altieri S Bortolussi S Ferrari C Clerici AM Zonta C Carraro F Filippi I Giorgi G Donati A Ristori S Vomero S Concas A Biggio G 《Bioconjugate chemistry》2010,21(12):2213-2221
Potential boron neutron capture therapy (BNCT) agents have been designed on the basis of the evidence about translocator protein (TSPO) overexpression on the outer mitochondrial membrane of tumor cells. The structure of the first TSPO ligand bearing a carborane cage (compound 2d) has been modified in order to find a suitable candidate for in vivo studies. The designed compounds were synthesized and evaluated for their potential interaction with TSPO and tumor cells. In vitro biological evaluation showed in the case of fluoromethyl derivative 4b a nanomolar TSPO affinity very similar to that of 2d, a significantly lower cytotoxicity, and a slightly superior performance as boron carrier toward breast cancer cells. Moreover, compound 4b could be used as a 1?F magnetic resonance imaging (MRI) agent as well as labeled with 11C or 1?F to obtain positron emission tomography (PET) radiotracers in order to apply the "see and treat" strategy in BNCT. 相似文献
145.
146.
Cliff C. Cheng Gerald W. Shipps Zhiwei Yang Noriyuki Kawahata Charles A. Lesburg José S. Duca Jamie Bandouveres Jack D. Bracken Chuan-kui Jiang Sony Agrawal Eric Ferrari H.-C. Huang 《Bioorganic & medicinal chemistry letters》2010,20(7):2119-2124
SAR exploration from an initial hit, (S)-N-(2-cyclohexenylethyl)-2-fluoro-6-(2-(1-hydroxy-3-phenylpropan-2-ylamino)-2-oxoethoxy)benzamide (1), identified using our proprietary automated ligand identification system (ALIS),1 has led to a novel series of selective hepatitis C virus (HCV) NS5B polymerase inhibitors with improved in vitro potency as exemplified by (S)-2-fluoro-6-(2-(1-hydroxy-3-phenylpropan-2-ylamino)-2-oxoethoxy)-N-isopentyl-N-methylbenzamidecarboxamide (41) (IC50 = 0.5 μM). The crystal structure of an analogue (44) was solved and provided rationalization of the SAR of this series, which binds in a distinct manner in the palm domain of NS5B, consistent with biochemical analysis using enzyme mutant variants. These data warrant further lead optimization efforts on this novel series of non-nucleoside inhibitors targeting the HCV polymerase. 相似文献
147.
Giselle?L?Ferrari Jefferson?LB?Marques Rajiv?A?Gandhi Simon?R?Heller Fábio?K?Schneider Solomon?Tesfaye Humberto?R?GambaEmail author 《Biomedical engineering online》2010,9(1):26
Background
Autonomic neuropathy is a common and serious complication of diabetes. Early detection is essential to enable appropriate interventional therapy and management. Dynamic pupillometry has been proposed as a simpler and more sensitive tool to detect subclinical autonomic dysfunction. The aim of this study was to investigate pupil responsiveness in diabetic subjects with and without cardiovascular autonomic neuropathy (CAN) using dynamic pupillometry in two sets of experiments. 相似文献148.
M Alonso N Alonso Rodriguez C Garzelli M Martínez Lirola M Herranz S Samper MJ Ruiz Serrano E Bouza D García de Viedma 《BMC microbiology》2010,10(1):151
Background
The Beijing lineage of Mycobacterium tuberculosis is causing concern due to its global distribution and its involvement in severe outbreaks. Studies focused on this lineage are mainly restricted to geographical settings where its prevalence is high, whereas those in other areas are scarce. In this study, we analyze Beijing isolates in the Mediterranean area, where this lineage is not prevalent and is mainly associated with immigrant cases. 相似文献149.
Giuseppina Sandri Maria Cristina Bonferoni Silvia Rossi Franca Ferrari Cinzia Boselli Carla Caramella 《AAPS PharmSciTech》2010,11(1):362-371
The aim of this paper was to evaluate the penetration enhancement properties of nanoparticles (NP) based on N-trimethyl chitosan (TMC 35% quaternization degree) loaded with insulin. The permeation performances of TMC NP were compared
with those of chitosan (CS) NP and also with TMC and CS solutions. To estimate the mechanism of penetration enhancement, two
different approaches have been taken into account: an in vitro study (Caco-2 cells) and an ex vivo study (excised rat duodenum, jejunum, and ileum). Insulin-loaded CS and TMC NP had dimensions of about 250 nm and had high
yield and high encapsulation efficiency. The in vitro study evidenced that TMC and CS were able to enhance insulin permeation to the same extent. Penetration enhancement properties
of TMC NP seem to be prevalently related to endocytosis while the widening of tight junctions appeared more important as mechanism
in the case of CS NP. The ex vivo study put in evidence the role of mucus layer and of its microclimate pH. In duodenum (pH 5–5.5), CS and TMC solutions were
more effective than NP while TMC NP were more efficient towards jejunum tissue (pH 6–6.5) for their high mucoadhesive potential.
Confocal laser scanning microscopy study supported the hypothesis that penetration enhancement due to TMC NP was mainly due
to internalization/endocytosis into duodenum and jejunum epithelial cells. The good penetration enhancement properties (permeation
and penetration/internalization) make TMC NP suitable carriers for oral administration of insulin. 相似文献