In this paper we report the synthetic procedures providing the C-substitution of the cobalt bis(dicarbollide) sandwich anion [(1,2-C2B9H11)-3,3′-Co]− with primary, secondary and tertiary alkylamine groups of different length of the aliphatic spacer attached to the carbon C(1) or C(1) and C(1′)...

Metal-free and metallo-porphyrazines having eight 5-hydroxypentylthio units at the peripheral positions have been prepared from 2,3-bis(5-hydroxypentylthio)maleonitrile. By the esterification reaction of magnesium hydroxy-porphyrazine with 3,4,5-tris(benzyloxy)benzoic acid in dicyclohexylcarbodi...

The electroreductive intermolecular coupling of aromatic ketones and aldehydes with α,β-unsaturated esters in the presence of TMSCl gave the adducts as γ-trimethylsiloxy esters. The detrimethylsilylation of the adducts with TBAF afforded 5-aryl substituted γ-butyrolactones. The electroreduct...

Anabolic androgenic steroids and high testosterone doses have been reported to induce impulsive behavior in man and behavioral disinhibition in rats. The purpose of the present study was to investigate whether aromatization of testosterone to estradiol is of importance for the behavioral disinhi...

Selective inhibition of both cyclooxygenase-2 (COX-2) and 15-lipooxygenase (15-LOX) may provide good strategy for alleviation of inflammatory disorders while minimizing side effects associated with current anti-inflammatory drugs. The present study describes the synthesis, full characterization ...

Ortho/para-aminobenzoic acids and corresponding methyl esters were selected as the diazo components to couple with two mono functional group transformation (FGT) precursors with different pyridine N-substituted groups [1-ethyl-6-((3-methoxypropyl)amino)-4-methyl-2-oxo-1,2-dihydropyridine-3-carbo...

The electroreduction of aromatic β-dimethylcarbamoyl-β-imino esters, prepared from (S)-aspartic acid, in the presence of chlorotrimethylsilane gave five-membered cyclized products, 1-benzoyl-4-hydroxy-5-aryl-N,N-dimethylpyrrolidine-2-carboxamides and 5-(dimethylcarbamoyl)-2-aryl-1H-pyrrol-3-yl...

Based on a model amidation reaction of benzoic acid triethylene glycol (TEG) ester with lithium anilide, which proceeded as rapidly as that of the methyl ester and faster than that of the ethyl ester, we considered that a TEG ester AB2 monomer would have sufficient reactivity to undergo chain-gr...

A series of 1,6-bis[(benzyloxy)methyl]uracil derivatives combining structural features of both diphenyl ether and pyridone types of NNRTIs were synthesized. Target compounds were found to inhibit HIV-1 reverse transcriptase at micro- and submicromolar levels of concentrations and exhibited anti-...

The diastereoselectivity in the triethylamine-catalyzed sulfa-Michael addition of nitroalkenes and thiols was investigated. The sulfa-Michael addition is kinetic control at the beginning and thermodynamic control at the end for less bulky reactants. Thus, kinetic and thermodynamic-controlled add...

The unprecedented annulation/hydroxyfluorination of propargylic carbamates to give 4-fluoromethyl-4-hydroxy-oxazolidinones was investigated. The reaction was effectively promoted by NaHCO3 and/or silver catalysis. The peculiar behavior of propargylic carbamates bearing a chiral steroidal moiety ...

The compounds [fac-Re(CO)3Cl(L)] and [M(CO)4(L)], M = Cr, Mo, W and L = 1,2-bis[(2,6-diisopropylphenyl)imino]acenaphthene, have been studied electrochemically and spectroelectrochemically (IR, UV–vis-NIR, EPR). The neutral rhenium complex contains an isopropyl-shielded chloride ligand; its reve...

Lanthanide triiodides LnI3 (Ln = Nd, Sm) were synthesized by an improved method and used for the synthesis of complexes with β-diketiminate (nacnac) ligand [Ln(LDipp)I2(THF)2] (LDipp = HC(C(NDipp)Me)2−, Dipp = 2,6-Diisopropylphenyl; Ln = Nd, 1a; Sm, 1b). These complexes were crystallized as sol...

Supramolecular self-assembly of amyloidogenic peptides is closely associated with numerous pathological conditions. For instance, Alzheimer´s disease (AD) is characterized by abundant amyloid plaques originating from the proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-...

Diacylglycerol acyltransferase 1 (DGAT1) is known to play an important catalytic role in the final step of triglyceride biosynthesis. High fat diet fed DGAT1 knockout mice were resistant to weight gain and exhibited increased insulin and leptin sensitivity thereby indicating a plausible role for...

Substituted (±)-trans-1-benzyl-6-oxo-2-phenylpiperidine-3-carboxamides (type I) and the acylated derivatives of (±)-trans-5-amino-1-benzyl-6-phenylpiperidin-2-one (type II) were prepared by the reaction of (±)-trans-1-benzyl-6-oxo-2-phenylpiperidine-3-carboxylic acid and some common reagents ...

The highly purified exo-β-N-acetylglucosaminidase (β-2-acetamido-2-deoxy-d-glucoside acetamidodeoxyglucohydrolase (EC 3.2.1.30) of Bacillus subtilis B has a pH Optimum of 5.9 and is most stable at 8.5. Its isoelectric point appears to be pH 3.8 and it has a mol. wt of about 75 000. The results...

The glycosylating activity of 2-methyl-glyco[1′,2′:4,5]- 2-oxazolines has been investigated in connection with the synthesis of 1,2-trans-2-acetamido-2-deoxy-glycosides. Treatment of 2-methyl-4,5-(3,4,6-tri-O-acetyl-2-deoxy-α-D-glucopyrano)-2-oxazoline (1) and 2-methyl-4,5-[4-O-(2-acetamido-3...

This study was undertaken to determine whether interactions of toxicologic importance might occur during combined exposure of male mice to 2-sec-butylphenyl N-methylcarbamate (BPMC) and O,O-dimethyl O-(3-methyl-4-methylthiophenyl)phosphorothioate (fenthion). The equitoxic coadministration of BPM...

We investigated noncholinergic actions of 2-sec-butylphenyl N-methylcarbamate (BPMC) on the isolated rabbit thoracic aorta to help determine the mechanisms responsible for its unique toxicological properties, which are characterized by cardiovascular collapse and low lethality compared to its an...