6320-16-7Relevant academic research and scientific papers
PROCESS FOR PREPARATION OF VORTIOXETINE HYDROBROMIDE
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Page/Page column 52-53, (2017/03/14)
The present invention provides a process for preparation of Vortioxetine hydrobromide (I). The present invention also relates to the novel intermediate and its use in preparation of vortioxetine hydrobromide (I).
INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 35, (2012/01/03)
Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
Bifunctional ligands based on the DOTA-monoamide cage
Barge, Alessandro,Tei, Lorenzo,Upadhyaya, Dharita,Fedeli, Franco,Beltrami, Lorena,Stefania, Rachele,Aime, Silvio,Cravotto, Giancarlo
experimental part, p. 1176 - 1184 (2008/10/09)
Efficient routes to DOTA-monoamide ligands bearing amino, hydroxyl, aldehyde and maleimido groups are described. These functional groups, which can be spaced at will from the coordination cage, will readily react with suitable groups of targeting moieties
An efficient chemoenzymatic synthesis of the bactericide lapyrium chloride
Rustoy, Eduardo M.,Baldessari, Alicia
, p. 4628 - 4632 (2007/10/03)
An efficient route for large-scale preparation of lapyrium chloride, a broad-spectrum antimicrobial surfactant, was developed from chloroacetic acid in four steps, three of them enzymatic. Due to the chemoselective behavior of the biocatalysts, lapyrium chloride was obtained in a high degree of purity and yield, from mild reaction conditions and following a low environmental impact methodology. Wiley-VCH Verlag GmbH & Co. KGaA, 2005.
Synthesis, spectral studies and anti-inflammatory activity of glycolamide esters of niflumic acid as potential prodrugs
Gadad, Andanappa K.,Bhat, Shailija,Tegeli, Varsha S.,Redasani, Vivek V.
, p. 817 - 821 (2007/10/03)
In order to reduce the gastric irritation caused by direct contract mechanism of the carboxylic acid group, a series of glycolamide esters of niflumic (CAS 4394-00-7) (1) have been prepared as biolabile prodrugs by reacting appropriate 2-chloroacetamides with niflumic acid. The required 2-chloroacetamides were obtained by the condensation of chloroacetyl chloride and corresponding amine. Their structures were confirmed by UV, IR and 1H NMR spectra. Selected compounds were evaluated for anti-inflammatory activity in carrageenan induced paw oedema in rats at the doses of 45, 90 and 150 mg/kg b.w. Prodrugs showed comparable anti-inflammatory activity (67.1-79.4%) at 150 mg/kg b.w. with respect to niflumic acid (70.3%) at 45 mg/kg b.w., indicating moderate release of niflumic acid in vivo. The highest activity was observed with diethylamine (4) and pyrrolidine (9) derivatives.
Inhibition of tumor cell growth by a specific 6-phosphofructo-2-kinase inhibitor, N-bromoacetylethanolamine phosphate, and its analogues.
Hirata,Watanabe,Miura,Ijichi,Fukasawa,Sakakibara
, p. 2047 - 2052 (2007/10/03)
The high rate of glycolysis despite the presence of oxygen and mitochondria in tumor cells implies an important role for this process in cell division. The rate of glycolysis is assumed to be dependent on the cellular concentration of fructose 2,6-bisphosphate, the concentration of which in turn depends on a bifunctional enzyme and the ratio of this enzyme's 6-phosphofructo-2-kinase versus its fructose 2,6-bisphosphatase activities. To prove the hypothesis that inhibition of glycolysis in tumor cells by 6-phosphofructo-2-kinase inhibitors would cause inhibition of tumor cell proliferation, ten N-bromoacetylethanolamine phosphate analogues were designed, synthesized, and tested. They were screened for their activities against various human tumor cell lines to study the effects of inhibition of glycolysis on cell proliferation. The relationship between the structure of these compounds and their inhibitory activity on cell proliferation was also discussed. It was found that the activity of N-(2-methoxyethyl)-bromoacetamide, N-(2-ethoxyethyl)-bromoacetamide, and N-(3-methoxypropyl)-bromoacetamide was comparable to that of the positive control AraC. These three inhibitors showed in vivo anticancer effects in P388 transplant BDF1 mice.
Substituted heteroaralkyl, heteroaralkenyl or halomethyl fungicides
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, (2008/06/13)
Compounds of the formula: STR1 wherein R is phenyl or phenyl substituted with 1 to 4 of the same or different substituents selected from fluoro, chloro, bromo, iodo, lower alkyl and trihalomethyl; R1 is lower alkyl; Y is lower alkenyl substituted with a 5- or 6-member heterocyclic ring containing 1 to 3 nitrogen atoms and the remainder of the ring atoms carbon atoms, or --CH2 W wherein W is fluoro, chloro, bromo, iodo, or a 5- to 6-member heterocyclic ring containing 1 to 3 nitrogen atoms and the remainder of the ring atoms carbon atoms; and X and Z are independently sulfur or oxygen; are effective fungicides.
