Phenmedipham strongly inhibits the electron transfer through PSII (50% inhibition at 0.02 μM). Its affinity for thylakoids is high (Km = 0.137 μM). A Km value of 0.067μM could be estimated for its specific binding to the D-1 protein. Diuron could replace phenmedipham on this target for which ...
The screening of known medicinal agents against new biological targets has been shown to be a valuable approach for revealing new pharmacology of marketed compounds. Recently, carbamate, urea and ketone inhibitors of fatty acid amide hydrolase (FAAH) have been described as promising treatments f...
Publisher SummaryThis chapter provides the basic synthesis paths routes for the manufacture of phenmedipham, with a listing of the main raw materials and intermediates used in the synthesis of phenmedipham. Phenmedipham is commercially known as Betanal and it belongs to the carbamate group.
Fatty acid amide hydrolase (FAAH) inhibitors have gained attention as potential therapeutic targets in the management of neuropathic pain. Here, we report a series of pyrazole phenylcyclohexylcarbamate derivatives standing on the known carbamoyl FAAH inhibitor URB597. Structural modifications le...
N-Monoalkyl and N,N-dialkyl carbamate prodrugs of naltrexone (NTX), an opioid antagonist, were synthesized and their in vitro permeation across human skin was determined. Relevant physicochemical properties were also determined. Most prodrugs exhibited lower melting points, lower aqueous solubil...
We have explored the synthesis of compounds that have good affinity for both μ- and δ-opioid receptors from the (αR,2S,5S) class of diaryldimethylpiperazines. These non-selective compounds were related to opioids that have been found to interact selectively with μ- or δ-opioid receptors as ...
N-Methyl- and N-phenylethyl-(±)-1,2,3,4,4a,5,10,10a-octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines (4 and 5, respectively) were found to be pure opioid antagonists. These compounds were shown to share many of the characteristics identified with the N-methyl- and N-phenylethyl t...
The widespread occurrence of ethyl carbamate (EC, 89.09 Da), a group 2A carcinogen, in fermented foods and alcoholic beverages has raised worldwide public health concern. Immunoassay for EC is unavailable due to the simple and small structure of EC. In this work, an initial attempt to produce an...
A sequential oxidative approach was designed to functionalize salicylaldehyde derivatives and provide corresponding bi-functional amide-carbamate and amide-quinone units. A combination of metal/metal free conditions and TBHP as the external oxidant provided the products in moderate to excellent ...
This current study described the design and synthesis of a series of derivatives based on a natural pyranoisaflavone, which was obtained from the seeds of Millettia pachycarpa and displayed attractive BChE inhibition and high selectivity in our previous study. The inhibitory potential of all der...
A deep revision of the carbamate methyl derivatization reaction with sodium hydride/dimethyl sulfoxide/methyl iodide was carried out. Representative carbamates, R1–NH–COO–R2, mainly N-methyl and N-aryl ones, have been studied in order to clarify which carbamates undergo this reaction. Two pos...
The potent and selective KOR antagonist JDTic was derived from the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of pure opioid antagonists. In previous studies we reported that compounds that did not have a hydroxyl on the 3-hydroxyphenyl group and did not have methyl gro...
To discover multifunctional agents for the treatment of Alzheimer's disease (AD), a series of chalcone-O-carbamate derivatives was designed and synthesized based on the multitarget-directed ligands strategy. The in vitro biological activities were evaluated including AChE/BChE inhibition, M...
3,3′-Bicyclopropenyl (1) was synthesized from a new isomer 3 of 1-chloro-2-(2-chloro-3-trimethylsilylcycloprop-1-yl)-3-trimethylsilylcyclopropanes, which was formed by ene dimerization of 1-chloro-3-trimethylsilylcyclopropene (2) followed by reduction with diimide. Compoumd 2 was generated by d...
(1- and trans-2-bromovinyl)trimethylsilane react rapidly with lithium in ether, however, dehydrohalogenation and coupling reactions preclude good yields of the lithium reagent. In situ trapping with excess trimethylchlorosilane yields trans-bis(trimethylsilyl)ethylene and demonstrates >80% conve...
Coupling reactions of (1-bromovinyl)trimethylsilane (1) with organozinc bromides catalyzed by tetrakis(triphenylphosphine)palladium(0) give not only the expected 1-substituted vinylsilanes (2) but also the isomeric 2-substituted vinylsilanes (3).
The excretion of aluminium in urine was significantly increased after intake of analgesics containing aluminium, confirming increased absorption and hence exposure to aluminium with such medication. The effect of aluminium on the kidney was further investigated by study of gene expression in mic...
The glycinate–guanidoacetate nickel (II) complex was synthesized and obtained as a crystalline powder. The characterization of this complex was performed by means of the experimental methods: CHN–O elemental analysis, atomic absorption spectrometry, thermo-gravimetric analysis and infrared spe...
A catalytic asymmetric synthesis of β-hydroxy-α-amino acid esters was developed using the direct aldol reaction of glycinate Schiff bases with aldehydes. The reaction was catalyzed by heterobimetallic asymmetric complexes without preformation of enol silyl ethers from glycinate Schiff bases. a...
Aluminum salts or doses that are unlikely in the human system have been employed in toxicity studies and much attention had been focused on the secondary target (neurons) of its toxicity rather than the primary target (astroglia). In order to address these issues, we have investigated the uptake...
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