Browsing by Subject "drug synthesis"
Now showing items 1-20 of 22
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1,2,3-Dithiazoles-new reversible melanin synthesis inhibitors: A chemical genomics study
(2015)A chemical genomic screen of an in-house library of small molecule heterocycles was carried out using Xenopus laevis embryos. This led to the identification of N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-4-methoxyaniline ...
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Cancer chemopreventive activity of brassinin, a phytoalexin from cabbage
(1995)Brassinin [3-(S-methyldithiocarbamoyl aminomethyl indole], a phytoalexin first identified as a constituent of cabbage, was synthesized and evaluated for cancer chemopreventive activity. Dose-dependent inhibition of ...
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The conversion of isothiazoles into pyrazoles using hydrazine
(2009)The conversion of isothiazoles into pyrazoles on treatment with hydrazine is investigated. The influence of various C-3, C-4 and C-5 isothiazole substituents and some limitations of this ring transformation are examined. ...
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Design, synthesis and biological evaluation of benzo[e][1,2,4]triazin-7(1H) -one and [1,2,4]-triazino[5,6,1-jk]carbazol-6-one derivatives as dual inhibitors of beta-amyloid aggregation and acetyl/butyryl cholinesterase
(2012)Alzheimer's disease (AD) onset and progression are associated with the dysregulation of multiple and complex physiological processes and a successful therapeutic approach should therefore address more than one target. Two ...
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Discovery of anti-cancer activity for benzo[1,2,4]triazin-7-ones: Very strong correlation to pleurotin and thioredoxin reductase inhibition
(2016)The thioredoxin (Trx)–thioredoxin reductase (TrxR) system plays a key role in maintaining the cellular redox balance with Trx being over-expressed in a number of cancers. Inhibition of TrxR is an important strategy for ...
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Fabrication, characterization, and evaluation in drug release properties of magnetoactive poly(ethylene oxide)-poly(l -lactide) electrospun membranes
(2013)The fabrication of electrospun magnetoactive fibrous nanocomposite membranes based on the water-soluble and biocompatible poly(ethylene oxide) (PEO), the biocompatible and biodegradable poly(l-lactide) (PLLA) and preformed ...
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Multistage nanoparticles for improved delivery into tumor tissue
(2012)The enhanced permeability and retention (EPR) effect has been a key rationale for the development of nanoscale carriers to solid tumors. As a consequence of EPR, nanotherapeutics are expected to improve drug and detection ...
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Novel lipophilic amidate oxorhenium and oxotechnetium complexes as potential brain agents: Synthesis, characterization and biological evaluation
(2001)Novel oxorhenium and oxotechnetium complexes based on the tetradentate 1-(2-hydroxybenzamido)-2-(pyridinecarboxamido)benzene, H3L, ligand have been synthesized and characterized herein. Thus, by reacting equimolar quantities ...
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A quorum sensing regulated small volatile molecule reduces acute virulence and promotes chronic infection phenotypes
(2011)A significant number of environmental microorganisms can cause serious, even fatal, acute and chronic infections in humans. The severity and outcome of each type of infection depends on the expression of specific bacterial ...
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Reinvestigating the synthesis of N-arylbenzamidines from benzonitriles and anilines in the presence of AlCl3
(2010)The preparation of N-phenylbenzamidine 3a from the reaction between benzonitrile Ia and aniline in the presence of AId3 is reinvestigated with respect to mode of reagent addition, reaction temperature and Lewis acid ...
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Ring transformations of 2-hydroxy-(4-chloro-5H-1,2,3-dithiazol-5-ylideneamino)arenes
(2015)Abstract The cyclisation reactions of 2-(4-chloro-5H-1,2,3-dithiazol-5-ylidene-amino)phenol (5a), 3-(4-chloro-5H-1,2,3-dithiazol-5-ylideneamino)pyridin-2-ol (5b) and 2-(4-chloro-5H-1,2,3-dithiazol-5-ylideneamino)pyridin-3-ol ...
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Structure based inhibitor design targeting glycogen phosphorylase b. Virtual screening, synthesis, biochemical and biological assessment of novel N-acyl-β-d-glucopyranosylamines
(2014)Glycogen phosphorylase (GP) is a validated target for the development of new type 2 diabetes treatments. Exploiting the Zinc docking database, we report the in silico screening of 1888 N-acyl-β-d-glucopyranosylamines ...
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Structure-activity relationships of brassinin in preventing the development of carcinogen-induced mammary lesions in organ culture
(1994)Brassinin, a pkytoalexin, is found in Chinese cabbage. Previously, we showed that brassinin significantly inhibited dimethylbenz(a)anthracene (DMBA)-induced mammary lesions in organ culture. Moreover, it was an effective ...
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Synthesis and study of the cancer cell growth inhibitory properties of α-, γ-tocopheryl and γ-tocotrienyl 2-phenylselenyl succinates
(2006)Vitamin E succinate selenium-conjugated molecules were synthesized and their apoptogenic properties were evaluated. 4-Methyl-2-phenylselenyl succinate (4) was prepared by the reaction of sodium benzeneselenolate with ...
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Synthesis of fused 1,2,4-dithiazines and 1,2,3,5-trithiazepines
(2014)Reacting ( Z)-N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-1H-pyrazol-5-amines 5 with Et2NH and then with concd H2SO4 gives 5H-pyrazolo[3,4-e ][1,2,4]dithiazine-3-carbonitriles 7 in good yields (74-85%) and 6H-pyrazolo-[3,4 ...
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The synthesis of pyrrolo[2,3-c][1,2,6]thiadiazine-5-carbonitriles from (4H-1,2,6-thiadiazin-4-ylidene)malononitriles
(2010)[3,5-Bis(dialkylamino)-4H-1,2,6-thiadiazin-4-ylidene]propanedinitriles 6a-c, react with sodium methoxide or ethoxide to give the corresponding 6-alkoxy-4-dialkylamino substituted pyrrolo[2,3-c][1,2,6]thiadiazine-5-carbonitriles ...
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Synthesis of sulfur containing analogues of the soluble guanylate cyclase inhibitor 8-bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one NS2028
(2011)Sulfur analogues of the soluble guanylate cyclase (sGC) inhibitor NS2028 1a are synthesized. Treating 8-bromo-2H-benzo[b][1,4]oxazin-3(4H)-one oxime (6) with 1,1′-thiocarbonyldiimidazole (1.1 equiv) gave the carbamothioate ...
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Synthesis, characterization and biological studies of new antimony(III) halide complexes with ω-thiocaprolactam
(2012)Three new antimony(III) halide complexes (SbX 3, X = Cl, Br and I) with the heterocyclic thione ω-thiocaprolactam (1-azacycloheptane-2- thione, (Hthcl)) of formulae {[SbCl 2(μ 2-Cl)(Hthcl) 2] n} (1), {[(SbBr 2(μ 2-Br)(Hthcl) ...
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A theoretical study of chlorine atom and methyl radical addition to nitrogen bases: Why do Cl atoms form two-center - Three electron bonds whereas CH3 radicals form two-center - Two-electron bonds?
(1996)Ab initio molecular orbital calculations have been carried out on a series of adducts between chlorine atom and NH3, NMe3, NCl3, HN=CH2, and pyridine, and between methyl radical and HN=CH2 and pyridine. A two-center-three-electron ...