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The urea derivatives a e were obtained from
2021-11-05

The urea derivatives 7a–e were obtained from 1-(3-phenoxybenzyl)-piperazine (6) by reaction of isocyanate, or triphosgene and subsequent reaction of produced carbamoyl chloride with the amine RH as shown in Scheme 2. The imidazole urea 7g was prepared by reaction of 6 with 1,1′-carbonyldiimidazole.
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br Dual acting HR antagonists While the
2021-11-05

Dual-acting HR antagonists While the present medicinal chemistry efforts are mainly focused on selective ligands targeting GPCRs, and particularly on H1R, H3R and H4R selective antagonists/agonists, there were and, also, still are several efforts to develop dual acting H1R/H2R, H1R/H3R and H3R/H4
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br Acknowledgements This work was supported
2021-11-05

Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom
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br Multiple sclerosis MS is an immune mediated disease of
2021-11-05

Multiple sclerosis MS is an immune-mediated disease of the human CNS with a pathological signature featuring immunocyte infiltration, altered cytokine production, oligodendroglial degeneration, astrogliosis, microglial activation, multifocal demyelination and axonal degeneration (Schipper, 2004b)
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The fibulins are a newly
2021-11-04

The fibulins are a newly abundantly in the basement membrane of blood vessels. Among them, fibulin-1 is essential for elastin polymerization. Tropoelastin cannot be assembled into mature elastin fibrils without the functional fibulin-1. In adult blood vessels, pronounced fibulin 1 deposition can be
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In addition researchers studying GPR
2021-11-04

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it CRT0044876 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex
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As the material for in silico experiments we
2021-11-04

As the material for in silico experiments we used an amino acetaminophen paracetamol sequence of a fragment of HIV1 surface glycoprotein gp120 corresponding to its less mutable B-cellular epitope: NMWKNNMVEQMHEDIISLWDQ. This sequence is the same as the sequence of the NQ21 and the biotin-NQ21 peptid
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Being a facultative intracellular pathogen C pseudotuberculo
2021-11-04

Being a facultative intracellular pathogen, C. pseudotuberculosis is exposed to oxygen and nitrogen species (ROS and RNS, respectively) reactive environment within macrophages (Nathan and Shiloh, 2000), apart from species endogenously generated by metabolic processes. These molecules interact with D
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br Membrane transporters as a novel therapeutic target in
2021-11-04

Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS
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Nuclear export of GK has been
2021-11-04

Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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Given the proposed importance of
2021-11-04

Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of A-1331852 binding, using changes in the enzyme's intrinsic fluorescence
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Although in in vitro analyses GANT sensitized Daoy cells
2021-11-04

Although in in vitro analyses GANT61 sensitized Daoy 2580 to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced within-group variatio
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Sickle erythrocytes are known to have an
2021-11-04

Sickle erythrocytes are known to have an increased adhesion to endothelial bcrp transporter (Hebbel et al., 1980, Hebbel et al., 1981a, Hebbel et al., 1981b, Wautier et al., 1985, Mohandas and Evans, 1987). Understanding the events associated with vaso-occlusion requires a detailed knowledge of the
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The highest metabolic stability observed for compound
2021-11-04

The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intraveno
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The F P concentration reported for
2021-11-04

The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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