1-O-cis-cinnamoyl-β-d-glucopyranose is one of the most potent allelochemicals isolated from Spiraea thunbergii Sieb. It is suggested that it derives its strong inhibitory activity from cis-cinnamic acid, which is crucial for phytotoxicity. It was synthesized to confirm its structure and bioacti...
4-Methyl- and 5-methyl-3-trimethylstannylcyclopentenes were obtained from bicyclo[3.1.0]hex-2-ene through hydrostannation. The four isomers were identified by chemical and physicochemical methods such as 90 MHz 1H FT NMR spectroscopy which gives some conformational information in the series of 5...
The gas chromatographic retention behaviour of C3C5 saturated branched-chain, C3C6 unsaturated, ethyl and 2-chloro-, 2,2-dichloro- and 2,2,2-trichloroethyl esters of benzoic, 4-nitrobenzoic and 3,5-dinitrobenzoic acids on SE-30 and OV-351 capillary columns at several temperatures is reported...
A new series of Zn(II), Cd(II) and Hg(II) complexes of (1E,5E)-1,5-bis(1-(pyridin-2-yl)ethylidene)carbonohydrazide (H2APC) have been prepared and characterized by elemental analyses, spectral (IR, UV–visible, mass and 1H NMR) as well as magnetic and thermal measurements. The data revealed that ...
A modified one-dimensional model (Premix) in conjunction with Chemkin II and a detailed kinetic scheme combining the chemistries of hydrogen, dimethyl ether and iso-octane combustion were used to investigate the effect of hydrogen addition on the chemical composition of laminar premixed dimethyl...
Bile acids (BAs) are endogenous steroids involved in the transport of lipids in bile, acting also as molecular signaling hormones. Primary BAs synthesized in the liver undergo several metabolic pathways in the intestine by gut microbiota to produce secondary BAs. Together with secondary BAs, oth...
The synthesis of four novel compounds, (i) [(11-{[2-(3-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]amino}-11-oxoundecyl)sulfanyl]acetic acid (4), (ii) N-[5-methyl-2-(3-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]undec-10-enamide (5), (iii) 2-[(11-{[5-methyl-2-(3-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]a...
The two nitroolefins, (Z)-1-(3-nitrophenyl)-4-phenylbut-1-ene and (Z)-1-(3-nitrophenyl)-5-phenylpent-1-ene, were stereospecifically prepared by Pd(0)-catalyzed cross-coupling reaction between (Z)-β-bromo-3-nitrostyrene and 2-phenylethyl- or 3-phenylpropyl zinc chloride, respectively. The yield ...
Chronic cholestasis and cholangitis may lead to the last phase known as biliary cirrhosis, characterized by cellular necrosis, apoptosis, tissue damage, local regeneration, inflammation and fibrosis. Such events are mediated by cytokines. Thalidomide and its analogs have shown to be effective im...
In the last two decades, trans-sialidase of Trypanosoma cruzi (TcTS) has been an important pharmacological target for developing new anti-Chagas agents. In a continuous effort to discover new potential TcTS inhibitors, 3-amino-3-arylpropionic acid derivatives (series A) and novel phthaloyl deriv...
Chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives were synthesized and their antibacterial activities were evaluated against fungus, Gram-negative and Gram-positive bacteria. In general, these compounds showed in vitro activities against all screened Gram-negative...
Based upon LX2421, a previously identified antiplatelet aggregation agent, a series of novel 2-amino-3-(naphth-2-yl)propanoic acid derivatives were designed, synthesized and evaluated. Among them, compounds LX14 and LX25 were identified as promising antiplatelet aggregation agents. The in vitro ...
A zwitterionic dimer model constructed of inter-molecular –N–H⋯O bonding has been proposed for the solid sample of DL-3-Aminoisobutyric acid consistent with IR absorption and Raman spectral features measured in the 3500–400/50 cm−1. This zwitterionic dimer model in water as solvent has been c...
Using a functional high-throughput screening (HTS) and subsequent SAR studies, we have discovered a novel series of non-nucleoside dengue viral polymerase inhibitors. We report the elaboration of SAR around hit compound 1 as well as the synthesis and antiviral evaluation of 3-phenyl-5-[(E)-2-(th...
A novel series of 2-amino-2-phenylethanol derivatives were developed as β2-adrenoceptor agonists. Among them, 2-amino-3-fluoro-5-(2-hydroxy-1-(isopropylamino)ethyl)benzonitrile (compound 2f) exhibited the highest activity (EC50 = 0.25 nM) in stimulating β2-adrenoceptor-mediated cellular cAMP p...
One unknown impurity (Imp-II) during the analysis of laboratory batches of isoproterenol hydrochloride was detected in the level ranging from 0.04% to 0.12% by high performance liquid chromatography with UV detection. The unknown impurity structure was proposed as 4-[2-(propan-2-ylamino)ethyl]be...
A sensitive gas chromatographic procedure for the determination of 7-methylbenz[c]acridines (7-methyl-BAcs) is presented. The 7-methyl-BAcs are easily oxidized to 7-formylbenz[c]-acridines (7-formyl-BAcs) with periodic acid in dimethyl sulfoxide. The 7-formyl-BAcs are then reacted directly with ...
The thiazolinone and phenylthiohydantoin derivatives of most amino acids can be hydrolyzed with alkaline dithionite to generate the free amino acid. The acidification of this hydrolysate with 3 n HCl containing thiodiglycol leads in the case of glutamic acid, glutamine, aspartic acid, asparagine...
The equilibrium solubility of barium iodate in water has been determined as 4.00, 5.38 and 8.20 (10-4 mol dm-3) at 2.0, 10.0 and 25.0 °C. A kinetic method which has been used for estimation of solubility is shown to be suspect.
Rationally designed asymmetrical alkylacyl phosphatidylcholines (APC) have been synthesized and evaluated as helper lipids for non-viral gene delivery. A long aliphatic chain (C22–C24) was introduced at the 1-position of glycerol backbone, a branched lipid chain (C18) at the 2-position, and a p...
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