The newly synthesized (α/β)-diastereomers of 6-(N-methyl-N-phenyl)aminomethylandrost-4-ene-3,17-dione (5) and 6-(N-methyl-N-phenyl)aminomethylandrost-4-en-17β-ol-3-one (6) were firstly investigated as substrates for the whole cells of Nocardioides simplex VKM Ac-2033D in comparison with their...

The melting point of an organic compound is commonly used for its characterization. In studies of 2-(aminomethyl)butanedioic acid, we found an apparent melting point that differed significantly from the literature values. Differential scanning calorimetry (DSC) revealed endothermic events prior ...

A series of N-substituted 1-aminomethyl-β-d-glucopyranoside derivatives was prepared. These novel synthetic compounds were assessed in vitro for inhibitory activity against yeast α-glucosidase and both rat intestinal α-glucosidases maltase and sucrase. Most of the compounds displayed α-gluco...

SummaryA homologous series of ω,ω,ω-triphenylalcohols and corresponding ω,ω,ω-triphenylalkyl-UDP derivatives was synthesized and tested as inhibitors of UDP-glucuronosyltransferase (UGT) activity in rat liver microsomes, with 1-naphthol, testosterone and bilirubin as substrates. Introducti...

A convenient synthesis of phosphonomethyl 1-O-(2,2,2-triphenyl)ethyl-α-D-gluco-2-heptulopyranosiduronate (2) is presented. The target compound proved to be an inhibitor of UDP-glucuronosyltransferase in vitro.

The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 μM, aq solubility

A conformationally constrained analogue 3 of the ACE inhibitor Idrapril has been prepared by a five-step synthesis. The key step in the synthesis is the desymmetrization of endo-norborn-5-ene-2,3-dicarboxylic anhydride 4 by reaction with t-butyl (S)-prolinate.

We assessed the effects of idrapril, a novel angiotensin-converting enzyme inhibitor, and captopril in the isolated rat heart after ischaemia and reperfusion and measured angiotensin-converting enzyme activity in myocardial tissue. Hearts were perfused and subjected to global ischaemia and reper...

The rapid discovery of a pharmacological chaperone toward human α-Gal A for the treatment of Fabry disease is described. Two polyhydroxylated pyrrolidines with the (3R,4S,5R) configuration pattern underwent rapid substituent diversity by conjugating the primary aminomethyl moiety of each with a...

Taking into account the high consumption of tomato and tomato-based products, a study of the occurrence of 7 nortropane alkaloids (calystegines A3, A5, B1, B2, B3, B4 and C1) in this type of matrix has been performed. For that purpose, a simple and fast solid-liquid extraction with methanol/wate...

A new synthetic route for formation of a central cycloheptanone intermediate leading to the nortropane alkaloid calystegine B2 is described. The approach installs the desired ketone functionality directly in a ring-closing metathesis step. The target compound was prepared over 10 steps from comm...

A palladium-catalyzed N-arylation of 1-substituted-1H-tetrazol-5-amines has been described for the first time. The reaction provides good yields of desired products with broad substrate scope and good functional group tolerance.

Heating of perfluorinated 1-methyl- and 1-ethyltetralins with SiO2 in an SbF5 medium at 100 °C results in perfluoro-4-alkyltetralin-1-ones formation. Perfluoro-4-methyltetralin-1-one, under the action of SbF5 at 180 °C with subsequent treatment of the reaction mixture with water, is converted ...

It was found that the reaction of mesomeric fluorocarbanions of the CF3CθXCOY type with benzoic anhydride leads to the loss of benzoyl fluoride and the formation of mesomeric carbanions of the FCOCθXCOY type. In a similar reaction with perfluorocarboxylic acid anhydrides, besides a CF3→COF tr...

The reaction of hemimellitic acid (1) with SF4/HF gives a 1 : 3.5 : 13 mixture of 1,2,3-tris (trifluoromethyl) benzene (2), 1,1,3,3-tetrafluoro 4-trifluoromethyl-l, 3-dihydroisobenzofuran (3) and 2,6-bis(trifluoromethyl)benzoyl fluoride (4). Treatment of the crude reaction mixture with aqueous K...

Herein we report the synthesis, PDE-4B and TNF-α inhibitory activities of a few dibenzo[b,d]furan-1-yl-thiazole derivatives. The hydroxycyclohexanol amide derivatives 14, 18, 24, 29, 31 and 33 exhibited promising in vitro PDE-4B and TNF-α inhibitory activities. Compound 24 showed good systemic...

There is an urgent need to develop new antibacterial agents because of multidrug resistance by bacteria and fungi. Schiff bases (aldehyde or ketone-like compounds) exhibit intense antibacterial characteristics, and are therefore, promising candidates as antibacterial agents. To investigate the m...

Recently, the phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) have been considered as promising targets for the treatment of cancer. Herein, we synthesized a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as novel PI3K/mTOR dual inhibitors for cancer the...

A convenient synthetic approach has been developed for 4-aryl-2,2′-bipyridine-6-carboxylic acids bearing long chained para-alkoxy residues at the 4-aryl substituents. These ligands have been further used for the preparation of neutral Eu(III), Tb(III), Sm(III) and Dy(III) complexes, and their p...

The synthesis and antiviral evaluation of a series of dihydropyrimidinone and thiopyrimidine derivatives bearing aryl α,γ-diketobutanoic acid moiety are described using the Biginelli multicomponent reaction as key step. The most active among 20 synthesized novel compounds were 4c, 4d and 5b, w...