An empirical approach proposed recently (Fluid Phase Equilibria, 434 (2017) 176–192) to distinguish different isomer molecules is extended in this paper aiming to apply for alkyl-esters. The vapor pressure, saturated liquid density of heavy unsaturated and branched alkyl-ester are predicted usi...
There are numerous chemotaxonomic studies on arthropods, but such are largely missing for millipedes. This appears curious since particularly in millipedes, the major taxa are clearly distinctive by different exocrine products, such as alkaloids (Glomerida), terpenoids (Polyzoniida), phenolics a...
A new one-pot synthesis of tetrasubstituted furans by the reaction between unsymmetrical alkynes and esters of carboxylic acids in the presence of EtAlCl2 and Cp2TiCl2 catalyst has been developed. The effect of the unsymmetrical alkyne substituent on the chemoselectivity of the reaction was studied.
Two new copper(II) complexes of formula [Cu2(2,5-dpp)(C2O4)2(H2O)4] (1) and [Cu2(2,5-dpp)(C5O5)2(H2O)4]·3H2O (2) [2,5-dpp = 2,5-bis(2-pyridyl)pyrazine, C2O42− = oxalate and C5O52− = croconate (dianion of 4,5-dihydroxycyclopent-4-ene-1,2,3-trione)] have been prepared and their structures determi...
Admicellar polymerization was used to modify surface of a cotton fabric in order to improve its ultraviolet protection property. A UV-absorbing agent, 2,4-dihydroxybenzophenone, was covalently bonded to a monomer, acryloyl chloride, and the product, 2-hydroxy-4-acryloyloxybenzophenone (HAB), was...
A synthetic procedure for the preparation of [18F]FPCBT, an imaging agent for the dopamine transporter (DAT), has been developed. The radiosynthesis was carried out in a two step procedure. Even though the yield was low, we were able to prepare 20 to 30mCi of the product, which was enough for tw...
3-(3-[18F]Fluoropropyl)-6-nitroquipazine ([18F]FPNQ) as a 5-HT transporter imaging agents was designed, synthesized, and evaluated. FPNQ was selected due to its potent in vitro biological activity (Ki=0.32 nM) in rat brain cortical membranes. The 18F-labeled FPNQ was prepared by reaction of the ...
To visualize serotonin uptake sites by positron emission tomography (PET), N-(3-[18F]fluoropropyl)-paroxetine ([18F]FPP) (Fig. 1), a derivative of the selective serotonin uptake blocker paroxetine, was synthesized from 3-[18F]fluoropropyltosylate and paroxetine via a one-pot procedure. The rate ...
Cancer vaccines targeting patient-specific tumor neoantigens have recently emerged as a promising component of the rapidly expanding immunotherapeutic armamentarium. However, neoantigenic peptides typically elicit weak CD8+ T cell responses, and so there is a need for universally applicable vacc...
The clinical application of gene silencing is hindered by poor stability and low delivery efficiency of naked oligonucleotides. Here, we present the in vitro and in vivo behaviors of a rationally designed, ternary, self-assembled nanoparticle complex, consisting of an anionic copolymer, cationic...
Metformin hydrochloride is an orally administered biguanide which is an oral anti-hyperglycemic agent. It shows incomplete absorption from the gastrointestinal tract and the absolute bioavailability is 50–60% with relatively short plasma half-life of 1.5–4.5 h. In this study the host-guest com...
A validated and repeatable high performance liquid chromatography (HPLC) method with online evaporative light scattering (ELSD) was developed for the analysis of two sterols, stigmasterol, β-sitosterol and a stanol, stigmastanol, found to be common in many herbal formulations and health care su...
The stereospecificity of chloramphenicol isomers on the inhibition of several plant systems was investigated. l-Threo, d-erythro, l-erythro and the antibiotic d-threo-chloramphenicol were effective inhibitors of auxin-induced elongation, 14C-leucine uptake and 14C-leucine incorporation into the ...
Carbohydrates as multifunctional naturally occurred chiral products were used for the first time as chiral building blocks in Mn(III)–salen complexes as catalysts for the enantioselective epoxidation of alkenes. The pathways of the mild and efficient synthesis of a Mn(III)–salen complex and it...
4-[[3-(1,6-dihydro-6-oxo-9-purin-9-yl)-1-oxopropyl]amino]benzoic acid (AIT-082) is an hypoxanthine derivative that stimulates in vitro neurite outgrowth and the production of adenosine and neurotrophins from astrocytes. These effects may predict an in vivo neuroprotective activity of the drug. T...
Because working memory is the primary type of memory which is disrupted by Alzheimer's diseas and stroke and during aging, any therapeutic drug for these conditions should improve and/or restore working memory. The win-shift memory paradigm has been shown to be an excellent model of working...
AIT-082 is a novel, metabolically stable, derivative of the purine hypoxanthine. Addition of AIT-082 to cultured PC12 cells enhanced significantly nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells. These results suggest a cellular mechanism, the enhancement of NGF-action, that...
A phase 1, randomized, double-blind, placebo-controlled, dose escalation study of the purine derivative, AIT-082 (Neotrofin™, NeoTherapeutics) was conducted in mild Alzheimer's disease (AD) patients to evaluate multiple-dose safety, tolerability, and pharmacokinetics. Possible short-term ef...
Expedient synthesis of Co(II) and Ni(II) complexes contriving the general molecular formula [M(L1)2Cl2] have been exemplified, where L1 = 4-((3-ethoxy-2-hydroxy benzylidene)amino)-N-(pyridin-2-yl)benzenesulfonamide. The structural feature of the complexes has been deduced from elemental analysis...
Desynchronization of circadian rhythms is a hallmark of depression. The antidepressant agomelatine, which is an MT1/MT2 melatonin receptor agonist/5-HT2C serotonin receptor antagonist has advantages compared to the selective serotonin reuptake inhibitors as a circadian phase-shifting agent. The ...
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