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<abstract_text><p>New 2-amino-6-ethoxybenzothiazole derivatives were synthesized and tested for their influence on physical work capacity in mice. It was shown that a pyridylidene or furylidene radical on the amine or a formulatio...
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<abstract_text><p>New 2-amino-6-ethoxybenzothiazole derivatives were synthesized and tested for their influence on physical work capacity in mice. It was shown that a pyridylidene or furylidene radical on the amine or a formulation with carboxypentanoate were important for producing effective new 2-amino-6-ethoxybenzothiazole derivatives. These compounds were either more effective or comparable with the well-known actoprotectors metaprot and ladasten, which are used at significantly higher doses.</p></abstract_text>
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The thermal condensation of 3-(2-Furyl)acrolein with 2-Amino-6-ethoxybenzothiazole generated a new Schiff base, (1E,2E)-N-(6-ethoxybenzo[d]thiazol-2-yl)-3-(furan-2-yl)prop-2-en-1-imine (L), with general formula of C16H14N2O2S. Als...
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The thermal condensation of 3-(2-Furyl)acrolein with 2-Amino-6-ethoxybenzothiazole generated a new Schiff base, (1E,2E)-N-(6-ethoxybenzo[d]thiazol-2-yl)-3-(furan-2-yl)prop-2-en-1-imine (L), with general formula of C16H14N2O2S. Also, a series of lanthanide complexes of gadolinium, samarium, and neodymium (La–Lc) were synthesized utilizing acetonitrile as the solvent and triethylamine as a buffer and catalyst. Based on elemental analysis, mass spectroscopy, and FTIR analysis, all of the Bis-(1E,2E)-N-(6-ethoxybenzo[d]thiazol-2-yl)-3-(furan-2-yl)prop-2-en-1-iminetri-nitratolanthanide(III) complexes with the general formula [LnL2(NO3)3]·H2O are solids with a 21 molar ratio (ligand metal). Based on conductivity estimates, they are nonelectrolytes and monoatomic paramagnetic according to the magnetic moment measurements, and one mole of lattice water was found after thermal gravimetric measurements and FTIR analysis. Therefore, the lanthanide complexes show a ten-coordination structure with a deformed bicapped square antiprismatic. The Schiff base and its complexes were screened for their antimicrobial, antifungal, antioxidant, and antitumor properties. Their antimicrobial and antifungal activities were strong, and they also produced good antioxidant and antitumor effects.
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In the reaction of oxalic acid hydrazide with isocyanates, new derivatives of semicarbazide were obtained [I-XII]. Cyclization of these derivatives with an aqueous 2% sodium hydroxide led to formation of new derivatives of delta2-...
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In the reaction of oxalic acid hydrazide with isocyanates, new derivatives of semicarbazide were obtained [I-XII]. Cyclization of these derivatives with an aqueous 2% sodium hydroxide led to formation of new derivatives of delta2-1,2,4-triazolin-5-one [XIII-XXIV].
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Several synthetic combretastatin A4 (CA-4) derivatives were recently prepared to increase the drug efficacy and stability of the natural product isolated from the South African tree Combretum caffrum. A group of ten 3-amino-2-azet...
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Several synthetic combretastatin A4 (CA-4) derivatives were recently prepared to increase the drug efficacy and stability of the natural product isolated from the South African tree Combretum caffrum. A group of ten 3-amino-2-azetidinone derivatives, as combretastatin A4 analogues, was selected through docking experiments, synthesized and tested for their anti-proliferative activity against the colon cancer SW48 cell line. These molecules, through the formation of amide bonds in position 3, allow the synthesis of various derivatives that can modulate the activity with great resistance to hydrolytic conditions. The cyclization to obtain the 3-aminoazetidinone ring is highly diastereoselective and provides a trans biologically active isomer under mild reaction conditions with better yields than the 3-hydroxy-2-azetidinone synthesis. All compounds showed IC_(50) values ranging between 14.0 and 564.2 nM, and the most active compound showed inhibitory activity against tubulin polymerization in vitro, being a potential therapeutic agent against colon cancer.
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Nitroacetamidine undergoes a useful cyclocondensation with beta-diketones to produce substituted 2-amino-3-nitropyridines. Use of an acylpyruvate generates hitherto unreported 2-amino-3-nitropyridine-4-carboxylates. These may be c...
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Nitroacetamidine undergoes a useful cyclocondensation with beta-diketones to produce substituted 2-amino-3-nitropyridines. Use of an acylpyruvate generates hitherto unreported 2-amino-3-nitropyridine-4-carboxylates. These may be converted easily to functionalized imidazo[4,5-b]pyridines and oxazolo-[5,4-b]pyridines. [References: 31]
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The crystal structures of methyl and ethyl N-(2,3-dimethoxybenzyl)-N-(p-toluenesulfonyl)-2-phenyl-glycinates 4a and 4b respectively, have been determined by X-ray diffraction analysis. The presence of different alkyl ester groups ...
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The crystal structures of methyl and ethyl N-(2,3-dimethoxybenzyl)-N-(p-toluenesulfonyl)-2-phenyl-glycinates 4a and 4b respectively, have been determined by X-ray diffraction analysis. The presence of different alkyl ester groups in both molecules does not affect the geometry retaining a svnclinal conformation for the N atom and the O atom of the C=O group [N-C17-C18-O5 38.1(5)degrees for 4a and 33.3(4)degrees for 4b]. [References: 14]
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A novel synthetic method for methyl 5-substituted thiazole-4-carboxylates (5) by the reaction of methyl 3-substituted 3-bromo-2-isocyanoacrylates(BICA)(1) with hydrogen sulfide in the presence of triethylamine in N,N-dimethylforma...
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A novel synthetic method for methyl 5-substituted thiazole-4-carboxylates (5) by the reaction of methyl 3-substituted 3-bromo-2-isocyanoacrylates(BICA)(1) with hydrogen sulfide in the presence of triethylamine in N,N-dimethylformamide was explored, and the reaction mechanism was elucidated. [References: 15]
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Four 4-amino-quitiazolinc compounds, including 7-[3-(2-methoxyphenoxy)propoxy]-N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 7-[3-(4-methoxyphenoxy)propoxy]-N'-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 2-[3-{4-(3-chloropheny...
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Four 4-amino-quitiazolinc compounds, including 7-[3-(2-methoxyphenoxy)propoxy]-N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 7-[3-(4-methoxyphenoxy)propoxy]-N'-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 2-[3-{4-(3-chlorophenylamino)-6-methoxy-quinazolin-7-yloxy}piopoxy]benzaldehyde,4-[3-{4-(3-chlorophenylamino)-6-methoxyquinazolin-7-yloxy)propoxy]benzaldehyde, were synthesized from N-[5-(3-ch!oropropoxy)-2-cyano-4-methoxyphen-yl]-N',Nr-dimethylfonnamidine by cyclization and emeration. The yields of the compounds Illa-d were 70.3, 71.0, 45.5 and 50.2 %, respectively. Their structures were characterized by TR, 'H NMR, ,3C NMR, MS and elemental analysis.
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Syntheses of (3R)-[4,4,4-D-3]-L-valine, [N-15]-L-isoleucine and [N-15]-allo-isoleucine from homochiral 2-alkylated carboxylic acids are described, The approach involves a one-carbon homologation of the carboxylic acid to give the ...
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Syntheses of (3R)-[4,4,4-D-3]-L-valine, [N-15]-L-isoleucine and [N-15]-allo-isoleucine from homochiral 2-alkylated carboxylic acids are described, The approach involves a one-carbon homologation of the carboxylic acid to give the corresponding beta-substituted alpha-keto ester which is converted directly to the alpha-amino acid in a one-pot procedure involving two enzyme catalysed reactions (Candida cylindracea lipase to hydrolyse the ester and leucine dehydrogenase to catalyse the reductive amination of the ketone). This strategy may be simply adapted for the selective labelling of each site of the L-amino acid. [References: 16]
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