نتایج جستجو برای: pyridinyl
تعداد نتایج: 490 فیلتر نتایج به سال:
Spillage of cyst contents during surgical operation is the major cause of recurrence after hydatid cyst surgery. Instillation of a scolicidal agent into a hepatic hydatid cyst is the most commonly employed measure to prevent this complication. SB202190 is a pyridinyl imidazole derivative and is known to be a specific inhibitor of p38 MAPK. In the present study, the scolicidal effect of SB202190...
Methuosis is a form of nonapoptotic cell death characterized by an accumulation of macropinosome-derived vacuoles with eventual loss of membrane integrity. Small molecules inducing methuosis could offer significant advantages compared to more traditional anticancer drug therapies that typically rely on apoptosis. Herein we further define the effects of chemical substitutions at the 2- and 5-ind...
The role of pyridinium cations in electrochemistry has been believed known for decades, and their radical forms have been proposed as key intermediates in modern photoelectrocatalytic CO(2) reduction processes. Using first-principles density functional theory and continuum solvation models, we have calculated acidity constants for pyridinium cations and their corresponding pyridinyl radicals, a...
The second-order nonlinear response of two dyes adsorbed at the dodecane/water interface was investigated by surface second harmonic generation (SSHG). These dyes consist of the same chromophoric unit, 2-pyridinyl-5-phenyloxazole, with an alkyl chain located at the two opposite ends. The analysis of the polarization dependence of the SSHG intensity as usually performed points to similar tilt an...
The intrinsic conformational biases of individual amino acids and their interstrand side-chain-side-chain (SC-SC) interactions both contribute to the stability of beta-sheets. The relative magnitudes of these effects have been difficult to assess in the context of folded proteins, where tertiary contacts complicate the quantitative analysis of local effects. We now report the results of such an...
The discovery of aurora kinases as essential regulators of cell division has led to intense interest in identifying small molecule aurora kinase inhibitors for the potential treatment of cancer. A high-throughput screening effort identified pyridinyl-pyrimidine 6a as a moderately potent dual inhibitor of aurora kinases -A and -B. Optimization of this hit resulted in an anthranilamide lead (6j) ...
The addition of molecular iodine to solutions of te rtiary aliphatic amines in liquid sulphur dioxide is found to result in the formation of stable free radical oxidation in te r mediates. In triethylam ine solutions, oxidised under these conditions, arom atisation appears to take place to produce a pyridinyl radical. Radicals formed from N-ethyldim ethylam ine, N ,N -diethylm ethylam ine and ...
Liquid chromatography/mass spectrometry (LC/MS) has been applied to the analysis of triphenylboron, which has been produced as a substitute for organotin compounds, in water. Although commercial triphenylboron compounds are produced as pyridinyl complexes, the chemical form in water is supposed to be mainly triphenylboron after liberating pyridine. The triphenylborons were extracted from water ...
At recombinant human 5-hydroxytryptamine (5-HT)5-HT1A receptors expressed in Chinese hamster ovary cells (CHO-5-HT1A), 5-carboxamidotryptamine (5-CT), acted as a full agonist (relative to 5-HT = 100%) for stimulation of receptor-mediated [35S]-GTP gamma S (guanylyl 5'-[gamma-thio]-tryphosphate) binding. In contrast, spiperone inhibited basal [35S]-GTP gamma S binding by 30.2% (IC50 = 55.5 nM) i...
The a7 subtype of the nicotinic acetylcholine receptor (nAChR) is the target of studies aimed at identifying features that will lead to the development of selective therapeutics. Five arylidine anabaseines, three with pyridine rings and two with the pyrrole rings, were synthesized in 35–65% yield via aldol condensation. The compounds are homologs of benzylidine anabaseine and were chosen for sy...
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