The impact of various secondary and tertiary pharmacophores on in vitro potency of soluble epoxide hydrolase (sEH) inhibitors based on the unsymmetrical urea scaffold 1 is discussed. N,N′-Diaryl urea inhibitors of soluble epoxide hydrolase exhibit subtle variations in inhibitory potency dependi...
Efficient synthetic approaches to functionalized 5-(3-R-1-adamantyl)uracils and related compounds (R=OH, COOH, NH2, etc.) are described. The selective hydroxylation of the adamantane tertiary C–H bonds in 5-(1-adamantyl)uracils with H2SO4 in trifluoroacetic anhydride is used as the key step. Su...
The present critical review outlines the close relationship and mutual interplay between molecular recognition, active site considerations in enzyme catalysis involving organocatalysis via hydrogen bonding. These interconnections are generally not made although; as we demonstrated they are quite...
Incorporation of an adamantyl group in prototypical soluble expoxide hydrolase (sEH) inhibitors afforded improved enzyme potency. We explored replacement of the adamantyl group in unsymmetrical ureas and amides with substituted aryl rings to identify equipotent and metabolically stable sEH inhib...
N,N′-disubstituted urea-based soluble epoxide hydrolase (sEH) inhibitors are promising therapeutics for hypertension, inflammation, and pain in multiple animal models. The drug absorption and pharmacological efficacy of these inhibitors have been reported extensively. However, the drug metaboli...
Out of the prominent global ailments, tuberculosis (TB) is still one of the leading causes of death worldwide due to infectious disease. Development of new drugs that shorten the current tuberculosis treatment time and have activity against drug resistant strains is of utmost importance. Towards...
A series of soluble epoxide hydrolase (sEH) inhibitors containing 2-fluorophenyl fragment was developed. Inhibition potency of the described compounds ranges from 0.7 to 630.9 nM. 1-(Adamantan-1-ylmethyl)-3-(2-fluorophenyl) urea (3b, IC50 = 0.7 nM) and 1-(adamantan-2-yl)-3-(2-fluorophenyl) urea ...
Publisher SummaryThis chapter focuses on boron-11 nuclear magnetic resonance (NMR) spectroscopy. The theoretical considerations of boron-11 chemical shifts are presented in the chapter. Tercovalent boron compounds, including substituted boron halides and aminoboranes are described in the chapter...
Boron nitride (BN) thin films have attracted a great deal of interest in recent years for their mechanical, optical and electronic properties. Many physical as well as chemical vapour deposition processes have been explored for the synthesis of BN coatings, especially cubic boron nitride — whic...
Methods of synthesis of the title compounds are described. The most widespread and frequently used method is the reaction of an alkynyl metal derivative (usually an alkynyllithium or alkynylmagnesium, less frequently an alkynylstannane) with an appropriate halide to form the alkynyl–element bon...
Hexagonal boron nitride (hBN) monolayers have attracted considerable interest as atomically thin sp2-hybridized sheets that are readily synthesized on various metal supports. They complement the library of two-dimensional materials including graphene and open perspectives for van der Waals heter...
The molecular structures of Cl3SiNMe2 and F3SiNMe2 have been determined in the vapour phase by the sector microphotometer method of electron diffraction. Both molecules are found to possess planar heavy-atom skeletons, after a small correction for shrinkage. The principal bond lengths are: Si-Cl...
An organophosphate pesticide terbufos (S-t-butylthiomethyl-O,O-diethyl phosphorodithioate; TBF) has been extensively used as an insecticide. A sexual dimorphism in TBF toxicity was not reported and remains unclear. The objective of the work was to investigate the influence of TBF on sexual dimor...
During gas chromatography (GC), the matrix can deactivate the active site during the transport of the compound from the injector to the detector. This deactivation capacity varies among matrices, as it is dependant on the concentrations of the different constituent compounds of each matrix. Duri...
Publisher SummaryThis chapter provides the basic synthesis paths routes for the manufacture of terbufos, with a listing of the main raw materials and intermediates used in the synthesis of terbufos. Terbufos is commercially known as Counter and it belongs to the phosphorodithioate group.
The photocatalytic degradation of terbufos in aqueous suspensions was investigated by using titanium dioxide (TiO2) as a photocatalyst. About 99% of terbufos was degraded after UV irradiation for 90 min. Factors such as pH of the system, TiO2 dosage, and presence of anions were found to influenc...
Adsorption of Phorate and Terbufos onto four tropical soils was investigated in this study. It was found that the adsorption kinetics was fast and that the equilibrium was established within 6 h. Adsorption isothermal data could be well described by the Freundlich equation. It was demonstrated t...
ObjectiveThe identification of pesticides in postmortem samples can be challenging, especially when organophosphates compounds (OPs) are involved. OPs are unstable and share several common metabolites, namely dialkylphosphates (DAP). Through a fatal poisoning case caused by the ingestion of terb...
We have tuned the applications of gold nanoparticles (Au NPs) with nitro and hydroxy benzylindole-dithiocarbamate derivatives for simple and selective colorimetric detection of terbufos and thiacloprid insecticides in environmental samples. The nitro and hydroxy benzylindole-dithiocarbamate (NBI...
A normal-phase displacement chromatographic method has been developed for the preparative-scale separation of the enantiomers of 1,2-O-dihexadecyl-rac-glycerol-3-O-(3,5-dinitrophenyl)carbamate using the Pirkle-type covalently bonded naphthylalanine silica chiral stationary phase. The separation ...
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