Dual fluorescence and fast intramolecular charge transfer (ICT) is observed with 4-(diisopropylamino)benzonitrile (DIABN) in alkane solvents. The rate constant ka for the reaction from the locally excited (LE) to the ICT state has a value of 3.4×1011 s−1 in n-hexane at 25°C, with an activation...
The first diastereoselective cycloaddition of a nitrile oxide with a homoallylic alcohol is discussed. The reaction of benzonitrile oxide with the magnesium alkoxides of chiral homoallylic alcohols has been shown to proceed with good diastereoselectivity, favoring the syn isomer of the resulting...
A concise and versatile method for the preparation of 3-aminoindoles from 2-(disubstituted amino)-benzonitriles is described, and in situ functionalizations were illustrated.
3-Arylideneindolin-2-ones are an attractive structural class in drug development, including registered drugs and drug candidates for treatment of cancer, Alzheimer's disease, infections and others. While residues at C-5 and C-7 are easily introduced by electrophilic substitution reactions, ...
Interactions between some stable linear peptides with renin inhibitory activity and a multispecific transport system in the basolateral plasma membrane of liver cells was studied on cell suspensions. The peptides used in our experiments were taken up by liver cells and subsequently eliminated wi...
A series of dipeptide renin inhibitors employing a 2,3-disubstituted cyclopropane carboxamide at the P3 position of the molecule were prepared by coupling racemic(IS,2R,3R) 2-alkylsulfonyl-3-phenyl(or cyclohexyl)cyclopropanecarboxylic acid with the amino acid derivatives 11a–d. The individual d...
Two series of lupane-type triterpenoic acid derivatives were synthesized and evaluated for their inhibitory activity against HIV-1 replication in acutely infected H9 cells, based on the fact that betulinic acid (1) and dihydrobetulinic acid (9) were identified as anti-HIV agents. Among the deriv...
The three title radicals, 11a, 11b and 11c have been synthesised by oxidation of the corresponding carbanions with iodine. The radicals are red to purple air stable solids and their ir and esr spectra show considerable interaction between the unpaired electron and the carbonyl or cyano group.
Optically pure (R)-(1-naphthylmethyl)succinic acid could be efficiently prepared by a combination of optical resolution and racemization of the undesired enantiomer or by catalytic asymmetric reduction of (1-naphthylmethylene)succinic acid over a rhodium (I)-chiral phosphine complex. Highly chem...
A series of structurally related citric acid–ciprofloxacin conjugates was synthesised to investigate the influence of the linker between citric acid and ciprofloxacin on antibacterial activities. Minimum inhibitory concentrations (MICs) were determined against a panel of reference strains and c...
A rapid and simple method for the resolution of Z-γ,γ′-di-tert-butyl-D,L-carboxyglutamic acid methyl ester is described. The new procedure is based on the enzymatic enantioselective saponification of the methyl ester by the endoprotease papain. Using a simple HPLC protocol the enantiomeric ex...
The effects of thermooxidation of a phytosteryl/-stanyl and a phytostanyl fatty acid ester mixture on cholesterol micellarization were investigated using an in vitro digestion model simulating enzymatic hydrolysis by cholesterol esterase and subsequent competition of the liberated phytosterols/-...
The optical purity of products derived from enantioselective reactions of the benzophenone imine of glycine tert-butyl esters can often be improved by conversion to the N-Fmoc α-amino acid tert-butyl esters followed by simple recrystallization.
The reductive cyclization of N-oxoacyl ortho-bromoanilides to form 3-hydroxy-2-oxindoles under the conditions of palladium catalyzed hydrogenation is described. This work may be viewed as a prelude to intermolecular hydrogen-mediated Grignard-type reductive couplings of organic halides with carb...
This study was designed to compare the effects of β-adrenoceptor agonists formoterol and BRL 37344 on spontaneous contractions and the levels of cAMP and cGMP of myometrial strips isolated from timed-pregnant rats. Myometrial strips were obtained from term-pregnant Wistar albino rats (n = 12), ...
We investigated the relaxant effect of β2-adrenoceptor agonist formoterol and β3-adrenoceptor agonist BRL 37344 on bovine iris sphincter and ciliary muscle and measured cAMP and cGMP levels.Iris sphincter (n = 16) and ciliary muscle (n = 16) strips were mounted in organ baths and tested for ch...
Alterations in vascular responses to β-adrenoceptor agonists in normotensive pregnancy and pre-eclampsia are not fully understood. Thus, we studied changes in vasodilator responses to β2-adrenoceptor agonist formoterol and β3-adrenoceptor agonist BRL 37344 on umbilical arteries isolated from ...
Cellular coupling of beta3-adrenoceptors (β3-ADR) to potassium channels in myometrium is largely unknown. In vitro study was undertaken to unravel the presence of β3-adrenergic receptors (ADR) and the role of K+-channels in mediating β3-ADR-induced relaxation in isolated myometrial strips fro...
Deoxynucleoside 5-monophosphate N-glycosidase, DNPH1 is a member of the nucleoside 2-deoxyribosyltransferase (NDT) family. This enzyme catalyzes the hydrolysis of deoxynucleoside monophosphates into free nucleobase moieties and 2-deoxyribose 5-phosphates.The DNPH1 enzymatic activity was first de...
Deoxynucleoside 5-monophosphate N-glycosidase or DNPH1 (former name Rcl) is a nucleotide hydrolase whose expression in mammalian cancer tissues has been associated with its tumorigenic potential. Therefore, the enzyme has been studied principally in rat and human models. We found the correspondi...
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