An aryl-substituted isobenzofuran-1(3H)-one lead compound was identified from a high throughput screen designed to find inhibitors of the lymphocyte pore-forming protein perforin. A series of analogs were then designed and prepared, exploring structure–activity relationships through variation o...
The coupling of o-bromobenzoic acid with terminal alkynes using 10% Pd/C–Et3N–CuI–PPh3 as a catalyst system leads to the synthesis of (Z)-3-alkylidenephthalides as the major product along with the traces of isocoumarin when the reaction was performed in 1,4-dioxane. The methodology afforded a...
An efficient and practical one-pot synthesis of 3-substituted isoindolin-1-ones and isobenzofuran-1(3H)-ones has been developed under solvent free-conditions using non-toxic and cheap phenylboronic acid as excellent catalyst. This strategy involves the sequential two-step Mannich/lactamization c...
A convenient approach for the preparation of (1S,3′R,4′S,5′S,6′R)-5-chloro-6-[(4-ethylphenyl)methyl]-3′,4′,5′,6′-tetrahydro-6′-(hydroxymethyl)-spiro[isobenzofuran-1(3H), 2′-[2H]pyran]-3′,4′,5′-triol is developed. The targeted compound was synthesized from 2-bromo-4-methylbenzoic aci...
Alkyne-based regioselective functionalization is an important transformation method for the synthesis of a wide variety of organic products. In this work, a regioselective TBAI-mediated oxidative 5-exo-dig iodo-oxycyclization of 2-alkynylbenzamide is used for the synthesis of various isobenzofur...
Methods were developed for the chromatography of fatty acid methyl esters on urea-impregnated papers, thin layers and columns of urea and Celite. Fatty acids of cholesterol esters from beef liver were separated by clathrate chromatography into factions of unsaturated, branched chain saturated an...
The low polarity of Carcinolopin and its positive reaction to colour tests for sterols indicated that this substance might be a sterol ester. Cholesterol esters separated from beef liver lipids by silicic acid chromatography showed a stimulating effect on the incorporation of labelled algal prot...
A procedure is described for the quantitative determination of Carcinolipin (cholesterol 14-methylhexadecanoate) in 0.5-1 g samples of biological materials (blood serum and tissues). The material is extracted with chloroform-methanol 2:1, internal standards of cholesterol margarate and 14-methyl...
Carcinolipin, the carcinogenic lipid substance from egg-yolks, markedly stimulates the incorporation of labeled valine, phenylalanine and lysine into the proteins of isolated microsomes in the presence of cell sap. Also the carboxyl-activation of amino acids is greatly enhanced in the presence o...
The allo-bile acids are a subset of the family of steroidal detergents found in most vertebrates. Because there are no major biological feedstocks for isolation of the allo-bile acids, they must be synthesized from the abundant 5β-reduced isomers. Here we report a general set of methods for the...
Paraformaldehyde in a methanolic solution of KOH converts ketones into α-methoxymethylated and α- hydroxymethylated products. The method was tested on nine steroidal ketones. On prolonged treatment the ketones formed are reduced to alcohols.
3-Aminopropyl β-(1 → 6)-d-glucotetraoside has been synthesized from 3-benzyloxycarbonylaminopropanol and 6-O-acetyl-2,3,4-tri-O-benzoyl-d-glucopyranosyl trichloroacetimidate by successive attachment of one monosaccharide unit in total yield of 22%. Free aminopropyl glycoside was converted into...
New substituted 3-((1H-1,2,3-triazol-1-yl)methyl)-5-arylisoxazoles (aryl = Ph, p-Tol) and 2-(5-phenylisoxazol-3-yl)-5-(2-(1-((5-(p-tolyl)isoxazol-3-yl)methyl)-1H-1,2,3-triazol-4-yl)ethyl)-1,3,4-oxadiazole were synthesized by means of click-chemistry procedures. The obtained compounds were used a...
Acetic acid bacteria (AAB) are a group of microorganisms highly used in the food industry. However, its use can be limited by the insufficient information known about the nutritional requirements of AAB for optimal growth. The aim of this work was to study the effects of different concentrations...
The tyrosinase inhibitory and antioxidant activities of four nicotinic acid derivatives, namely, nicotinamide, methyl nicotinate, nicotinic acid hydroxamate (NAH), N-methyl nicotinic acid hydroxamate (NAH-M), and kojic acid, were studied. The tyrosinase inhibitory activity was found to follow th...
Structure and properties of a rare metal complex of the chiral Schiff base ligand derived from ortho-vanillin and L-tyrosine are presented. This study is a continuation of research on ligands containing biologically compatible moieties. The ligand is also fully characterized in form of a sodium ...
Acids, or acidulants as they are also called, are commonly used in food processing as flavor intensifiers, preservatives, buffers, meat-curing agents, viscosity modifiers, and leavening agents. This article discusses the functions that acidulants have in food systems and reviews the more commonl...
A newly isolated salt-tolerant alkaliphilic actinomycete, Nocardiopsis dassonvillei strain OK-18 grows on mineral salts medium with glucose as carbon source. It also grows and produces protease with amino acids as sole carbon source. The synthesis of extracellular alkaline protease parallel to g...
Novel 3-[4-(dimethylamino)phenyl]alkyl-2-oxindole analogs were synthesized by either of the following two pathways: (1) a sequence of Knoevenagel condensation of oxindole with (4-dimethylamino)cinnamaldehyde–hydrogenation, or (2) alkylation of oxindole dianion with [(4-dimethylamino)phenyl]alky...
The corrosion inhibitory action of a Schiff base, 4-{[4-(dimethylamino)benzylidene]amino}-5-methyl-4H-1,2,4-triazole-3-thiol (DBAMTT), on 316 stainless steel (316 SS) in 2M HCl was studied using potentiodynamic polarisation technique, electrochemical impedance spectroscopy(EIS) and weight-loss m...
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