Diethyl pyrocarbonate inactivated aldehyde reductase II (l-gulonate: NADP+ 6-oxidoreductase, EC 1.1.1.19) from human placenta. A concentration of 0.5–1.0 mM diethyl pyrocarbonate caused 40–65% loss of activity. The inactivation of the enzyme by diethyl pyrocarbonate was reversed by hydroxylami...

Kinetic and thermodynamic studies have been made on the effect of diethyl pyrocarbonate as a histidine modifier on the active site of adenosine deaminase in 50 mM sodium phosphate buffer pH 6.8, at 27°C using UV spectrophotometry and isothermal titration calorimetry (ITC). Inactivation of adeno...

Diethyl pyrocarbonate inactivates enoyl-CoA hydratase (l-3-hydroxyacyl-CoA hydro-lyase, EC 4.2.1.17) with a second-order rate constant of 1.3 M−1 ·s −1. Partial protection is given against inactivation by the substrate analogue acetoacetyl-CoA. The single histidine per enzyme subunit is complet...

Thymidylate synthase (5,10-methylenetetrahydrofolate: dUMP C-methyltransferase, EC 2.1.1.45) from Lactobacillus casei was inactivated by treatment with diethyl pyrocarbonate. The inactivation was apparently due to the modification of a large proportion of the enzyme's histidine residues. Ne...

Fast in situ forming thermosensitive hydrogels consisted of vinyl sulfone bearing p(HPMAm-lac1–2)-PEG-p(HPMAm-lac1–2) triblock copolymers and thiol modified hyaluronic acid were prepared via a dual cross-linking strategy based on thermal gelation at 37 °C and simultaneous Michael addition cro...

Photosensitive in situ cross-linked hyaluronan (HA) hydrogels are prepared by modular chemoselective assembly from the biopolymer precursors and novel heterobifunctional linkers with middle photo-labile ortho-nitrobenzyl group and orthogonally reactive terminals. Starting from the thiol-modified...

The reaction of 7-fluoro and 7-chloronorbornadiene with different diazoalkanes was studied in order to determine the respective influence of these halogens on the steric course of the cycloadditions. The endo attack is predominant with small diszocompounds even with fluorine as the C 7 halogen.

Binding of cationic surfactants to anionic polymers is well studied. However, the surfactant binding characteristics at very low concentration near the start of binding and at high concentration, where charge compensation may occur, are less well known. Therefore, the binding characteristics of ...

The effect of temperature on the thermodynamic parameters of micellization of a homologous series of n-alkylpyridinium chlorides has been studied by isothermal microcalorimetry. The decyl, dodecyl and tetradecyl compounds were studied both in water and in 0.1 M NaCl in the temperature range 6–6...

Aggregation in the aqueous solutions of decylpyridinium chloride, dodecylpyridinium chloride and tetradecylpyridinium chloride has been investigated by conductivity measurements at 20–40°C, and thermodynamic characteristics of micellization have been analysed.

Synthesis of dimeric nucleoside building with a N-cyanoguanidine linkage was performed by reaction of 3′-amino-3′-deoxythymidine with S,S-dimethyl-N-cyanodithioimidocarbonate followed by reaction of the obtained isothiourea with 5′-amino-2′,5′-dideoxynucleosides. These dimers were protected...

The isothermal synthetic method was used to measure CO2 solubilities in three high-boiling-point absorbents, such as 2-ethoxyethyl ether, 2-butoxyethyl acetate and 2-(2-ethoxyethoxy)ethyl acetate under pressures ranging from 0 to 1.3 MPa and temperatures ranging from 293.15 to 333.15 K. Henry&#x...

We recently reported the anti-cancer and anti-cytomegalovirus (CMV) activity of artemisinin-derived trioxane diphenylphosphate dimer 838. To probe the relationship between chemical structure and anti-CMV and anti-cancer activities, we now report synthesis and evaluation of a series of eight new ...

Manganese(III) acetate-based radical cyclizations of various fluorinated 1,3-dicarbonyl compounds with alkenes produced 3-fluoroacylated 4,5-dihydrofurans and 2-acetyloxy-2-fluoroalkylated tetrahydrofurans in good yields. Mechanism was proposed for the formation of all compounds. The radical cyc...

A novel efficient strategy for the synthesis of rare 7-methoxy-2-thioxo-2,3-dihydro-1H-1,3-diazepin-4(7H)-ones is described. Methanol, solvent for this one-step reaction, participated in this seven-membered ring closure reaction between nitroallylic acetates and thiourea. The thiourea itself als...

The first organocatalytic enantioselective cascade reaction of Morita–Baylis–Hillman acetates of nitroalkenes with pyrazolones has been developed. With 20 mol % of chiral tertiary-amine squaramide, 1,4,5,6-tetrahydropyrano[2,3-c]pyrazoles were afforded in moderate yields (up to 71%) with excel...

Betaine-type ligands are an attractive class of zwitterionic molecule, which have attracted considerable interest because they may not only keep the versatile coordination modes of carboxylate groups but also provide a new way to adjust the charge distribution of coordination polymers by cationi...

An efficient route for the synthesis of novel bis(1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile) derivatives is reported. The synthetic pathway involves one pot, synthesis of bis-aldehydes, malononitrile, and pyrazolone in the presence of pyridine. The anticancer activity of the synthesized pr...

A convenient synthesis of the symmetrical bis(difluoromethyl)-1,4-thiazine 1,1-dioxides was carried out via heterocyclization of bis(2,2,3,3-tetrafluoropropyl)sulfone with ammonia and primary amines. The reaction with excess of ammonia leads to the formation of 3,5-bis(difluoromethyl)-4H-1,4-thi...

Two novel series of N-2,3-bis(6-substituted-4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)naphthalene-1,4-diones 3a-d and substituted N-(methyl/ethyl)bisquinolinone triethyl-ammonium salts 4e,f were successfully synthesized. The synthesized compounds were targeted as new candidates to extracellular s...