The efficacy of closing cyclooctane rings via transannular metal-stabilized carbene insertion reactions within an 11-membered macrocyclic lactone ring was explored. The impact of performing these reactions in a transannular fashion was evaluated via a comparative study of closely analogous intra...

The multigram synthesis of N-protected 2-pyridone boronic acid derivatives via a [4+2] cycloaddition of alkynylboronates with 2-pyrazinones is presented. The reactions are highly chemoselective, and generally highly regioselective although trimethylsilyl-substituted alkynylboronates have proven ...

Isoform-selective inhibition of PI3K-α has been identified as one of the important strategy to discover effective and safer anticancer agents. Herein, we report discovery of ‘quinazoline’ as a new chemotype for isoform-selective PI3K-α inhibitors. The indolyl substituted quinazoline 9u displ...

Cereal-based fermented beverages are non-dairy products which are considered possible carriers for probiotic strains and alternatives for use by vegans and lactose-intolerant consumers. In the present work, the commercial probiotic, Lactobacillus paracasei LBC-81, was used singly and in co-cultu...

Single topical treatment with l-adrenaline bitartrate in eyes of albino rabbits gave a prompt concentration-related increase in pupil diameter, peak values occurring at 1–2 hr. Ocular tension decrease commenced 2–3 hr after treatment, at the same time that the mydriatic effect started to decli...

Series of new aromatic R2R′2N+Br− (R=benzyl, 4-methylbenzyl, 2-phenylethyl, 3-phenylpropyl; R′=ethyl, methyl, isopropyl) or RR′2NH+Br−-type (R=benzyl, R′=isopropyl) quaternary ammonium bromides were prepared by using novel synthetic route in which a formamide (N,N-diethylformamide, N,N-dimet...

Bis[dibenzyldimethylammonium]CuBr4, bis[dibenzyldimethylammonium]CuCl4 and bis[dimethyldi(2-phenylethyl)ammonium]CuBr4 were crystallized from acetonitrile and/or dilute HX solutions. Five different kinds of single crystals were obtained. In the case of bis[dibenzyldimethylammonium]CuX4 (X=Br or ...

Racemic complexes with the general formula cis-[MoO2(bzacLn)] (1–4) (H2bzacLn = 2-((4/5-R-2-hydroxyphenylamino)(pyridin-2-yl)methyl)-1-phenylbutane-1,3-dione, where n = 1–4 for R = H, 5-Me, 5-Cl and 4-Me, respectively and 2Hs represent the dissociable phenolic proton and the active tertiary CH...

Reactions of both diastereomeric vicinal bromofluorocyclohexanes with sodamide, sodium methoxide, potassium tert-butoxide, and triethylamine were studied. cis-1-Bromo-2-fluorocyclohexane eliminated almost exclusively hydrogen bromide giving mainly 1-fluorocyclohexene and a small amount of 3- flu...

The chemiluminescence reaction between an aryl oxalate, hydrogen peroxide and a fluorescent compound is well known for use in h.p.l.c. post-column reactors. Here, several aryl oxalates are evaluated for this purpose in terms of intensity, rate of chemiluminescence decay, solubility in different ...

Several new bis(pentafluorophenyl) nickel (II) complexes with O,O- and O,N-donor ligands were prepared by directly reacting the hydroxo-complex [{Ni(C6F5)2(μ-OH)}2]2− with the protic acids oxalic (H2ox), glycine (Hgly), picolinic (Hpic), 2-aminobenzoic (Hambz), acetohydroxamic (Haha) and benzoh...

The pre-chemiluminescent hydrogen peroxide-bis(2,4-dinitrophenyl) oxalate reaction has been studied in order to understand better its role in peroxyoxalate chemiluminescence. The reaction is shown to be first order in each reactant. An unusual biexponential degradation of the oxalate occurs whic...

The kinetics of the hydrolysis of bis(2,4-dinitrophenyl) oxalate (DNPO) were studied by infrared spectroscopy. The changes in the carbonyl region showed that neither 2,4-dinitrophenyl hydrogen oxalate nor oxalic acid could be detected. Simultaneously, the rate of evolution of carbon dioxide was ...

The emergence of multidrug-resistant bacteria has created an urgent need for antibiotics with a novel mechanism of action. The bacterial cell division protein FtsZ is an attractive target for the development of novel antibiotics. The benzo[c]phenanthridinium sanguinarine and the dibenzo[a,g]quin...

The oxidation chemistry of dopa in relation to melanin biosynthesis has been extensively studied. However, the oxidation of its lower homolog viz., 3,4-dihydroxyphenylglycine has not been described. Using 3,4-dimethoxybenzaldehyde as the starting material, the chemical synthesis of 3,4-dihydroxy...

Systemic acquired resistance (SAR) is a long lasting inducible whole plant immunity often induced by either pathogens or chemical elicitors. Salicylic acid (SA) is a known SAR signal against a broad spectrum of pathogens in plants. In a recent study, we have reported that benzoylsalicylic acid (...

The diethyl esters of cis- and trans-epoxysuccinic acid were synthesised and examined. The compounds were stable for short periods at pH 5·0, as determined by gas-liquid chromatography. Both compounds were non-toxic to mice, possibly being detoxified in the liver by conjugation with glutathione...

Response surface methodology, which allows for rapid identification of important factors and optimization of them to enhance enzyme production, was employed here to optimize culture conditions for the production of cis-epoxysuccinic acid hydrolase from Bordetella sp. strain 1–3. In the first st...

Purification of a cis-epoxysuccinic acid hydrolase was achieved by ammonium sulfate precipitation, ionic exchange chromatography, hydrophobic interaction chromatography followed by size-exclusion chromatography. The enzyme was purified 177-fold with a yield of 14.4%. The apparent molecular mass ...

Free and conjugated phenolic acids accumulate in the plasma in acute renal failure. Some glycine conjugates of substituted benzoic acids have been synthesized and the effects of the hippuric and corresponding benzoic acids on some rat-brain enzyme systems have been studied. Where the free acid i...