Most of traditional and contemporary interest in s-tetrazine derivatives focuses onto their redox properties, reactivity and energy density. In recent times, however, an increasing number of reports highlighted the possible usefulness of the s-tetrazine moiety as a binding site for anionic and e...
The ligand 6-methoxy-N,N-bis(pyridin-2-ylmethyl)-1,2,4,5-tetrazin-3-amine (L) has been prepared by nucleophilic substitution from 3-chloro-6-dipicolylamino-1,2,4,5-tetrazine (1). The ligand L, together with two neutral zinc(II) and cadmium(II) metal complexes, respectively formulated as [ZnLCl2]...
Two novel bipolar Ir(III) complexes named (Czppy)2Ir(tfmptz) and (Czppy)2Ir(pptz) were synthesized and characterized, where the Czppy is 9-(4-(pyridin-2-yl)phenyl)-9H-carbazole, tfmptz refers to 2-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)pyridine and Hpptz represents 2-(1H-tetrazol-5-yl)pyridi...
The synthesis is reported of the complexes [Rh- (CH3CO2)2L]2 where L = misonidazole, desmethylmisonidazole, 2-nitroimidazole-l-ethanol and 1-(2- hydroxy 3-methoxypropyl)-2-methyl-5-nitroimidazole (Roll-3696), and of the rhodium(II) butyrate analogues with the last two nitroimidazole ligands Crys...
1-Methyl-2-nitrosoimidazole (INO), the 2-electron reduction product of 1-methyl-2-nitroimidazole (INO;), was prepared by electrochemical reduction of INO2 to 2-hydroxylamino-1-methylimidazole (INHOH), followed by back oxidation with iodine. Although stable in crystalline form, INO reacted in wat...
2-Nitroimidazoles were introduced into radiation therapy to test their ability to radiosensitize hypoxic cells in solid human tumours. In addition, they are selectively reduced in hypoxic cells to form reactive metabolites that may be effective cytotoxins. 1-Methyl-2-nitroimidazole (INO2) was in...
The crystal structures of two similar 1-R-2-methyl-4-nitroimidazoles, where R is allyl (CH2–CHCH2, 1) and 2-bromoethyl (CH2–CH2Br, 2) have been determined by means of X-ray crystallography at 100(1) K. In both cases the compounds crystallize with two different (symmetry-independent) molecules ...
In this study, some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives were synthesized by reacting 2-(2-methyl-5-nitro-1H-imidazolyl)ethylamine dihydrochloride, which was prepared using metronidazole, with some 1,4-dicarbonyl compounds. The structure elucidation of the c...
The 2-nitroimidazoles have been used clinically to radiosensitize resistant hypoxic cells, but a dose-limiting peripheral neuropathy has restricted their therapeutic effectiveness. A model compound, 1-methyl-2-nitroimidazole (INO2), was used to investigate the possible role of oxidative stress i...
Two similar 4-nitroimidazole derivatives, 1-(2′-aminophenyl)-2-methyl-4-nitroimidazole, C10H9N3O3, and 1-(2′-hydroxyphenyl)-2-methyl-4-nitroimidazole, C10H10N4O2, crystallize with two molecules in the asymmetric unit (Z′ = 2). Packing conflicts may result from tendency towards closing hydroge...
The serotonin reuptake process is observed in the central nervous system and in cells derived from the neural crest. It would therefore be of great interest to visualize this reuptake for brain exploration and to visualize the tumors derived from these cells (Apudome). Fluvoxamine has been descr...
A novel class of modified 1,5-disubstituted tetrazoles was designed and synthesized, their biological activity as cyclooxygenases inhibitors was screened, and their molecular docking studies were performed. The structural modifications of the first category included the 4-methylsulfonyl phenyl a...
Fourteen new 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5-LOX with IC50 in the range of 0.10–9.87 μM. Particularly, 10f exhibited well balanced inhibitory action on these enzym...
Published methods of synthesizing chlorinated biphenyl methylsulfonys require the separation of a complex mixture of impurities and isomers using both normal and reverse phase HPLC. Even with semi-preparative scale equipment, the process is tedious and time-consuming. In this report, the palladi...
A novel series of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidine-based cyclooxygenase-2 (COX-2) inhibitors, which have a different arrangement of substituents compared to the more common 1,2-diarylheterocycle based molecules, have been discovered. For example, 2-(butyloxy)-4-[4-(...
An α-C(sp3)−H functionalization of alkyl nitriles under metal-free and neutral conditions is presented. In the presence of di-tert-butyl peroxide (DTBP), N-allyl anilines underwent exo-selective cyanoalkylation/cyclization cascade, providing a direct access to 3-cyanoalkyl indolines. Previously...
Three-component reaction of alkyl isocyanides and dialkyl acetylenedicarboxylates in the presence of 2,2,2-trifluoro-N-aryl-acetamides in dichloromethane at ambient temperature afforded dialkyl 2-(N-(aryl)-2,2,2-trifluoroacetamido)-3-(alkylimino) methylene-succinate derivatives in excellent yields.
Glutamate (GLU) associated with glycine, act as co-transmitter at the N-methyl-d-aspartate/glycine-B (NMDA/GLYB) receptor. Dorsal periaqueductal gray (dPAG) neurons express NMDA/GLYB receptors suggesting a GLU physiological role in mediating the responses elicited by stimulation of this area. Im...
ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic potential, but none of the described synthetic compounds has so far reached the market. To optimise the activities and physicochemical properties of our previously reported N-phenylpyrrolamide inhibitors, we hav...
For decades neuroreceptor research has focused on the development of NMDA glycine-site antagonists, after Johnson and Ascher found out in 1987 about the co-agonistic character of this achiral amino acid at the NMDA receptor. Contrary to the inhibitory glycine receptor (glycineA) the glycine bind...
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