The addition of one equivalent of 2-nitrobenzenesulfenyl chloride to 1-(dimethoxymethyl)-2,3,5,6-tetramethylidene-7-oxabicyclo[2.2.1]heptane (4) is highly regioselective giving 2-(chloromethyl)-1-(dimethoxymethyl)-5,6-dimethylidene-3-[(2-nitrophenylthio)methyl]-7-oxabicyclo[2.2.1]hept-2-ene (9)....

Methods for the conversion of 1,4,5-naphthalenetriols into the corresponding monomethoxy diacetates are described. All utilise the formation of peri-bridged intermediates.

We have adopted the application of two fluorescent indicator dyes to studying the viability of monolayers of primary rainbow trout hepatocytes. The two fluorescent dyes—Alamar blue, which indicates metabolic activity of a cell, and 5-carboxyfluorescein diacetate acetoxymethyl ester (CFDA-AM), w...

This paper deals with an extensive analytical approach, which uses two complementary tandem mass spectrometry techniques, to characterize the chlorogenic acids (CGAs) present in a typical Italian sweet cherry variety (cv Ferrovia). Sixteen monoacyl-quinic acids and esters, five diacyl-quinic aci...

In the search for new bioactive natural products, plant sources represent a particularly suitable starting point in drug discovery. Among natural products, phenolic derivatives have a prominent place with several compounds exhibiting remarkable activities. This paper described the phenolic compo...

Zatosetron (13 mg or 0.19 mg/kg), a potent and selective 5-HT3 receptor antagonist was studied with a 30 min infusion in a crossover double-blind placebo-controlled trial for acute migraine therapy. Groups receiving zatosetron and placebo were demographically similar and zatosetron was well-tole...

The inhibition of 5-lipoxygenase (5-LO), the key enzyme for the biosynthesis of leukotrienes (LTs), has generated increasing enthusiasm as anti-inflammatory and antitumor strategies in recent years. Based on our previous studies, we synthesized a series of dihydroxycinnamic acid-based analogs th...

New 4-{[5-arylidene-2-(4-fluorophenylimino)-4-oxothiazolidin-3-yl]methyl}benzoic acids (5) and 2-thioxo-4-thiazolidinone analogues (6) were synthesised as a part of a continuing search for new inhibitors of protein tyrosine phosphatase 1B (PTP1B), an enzyme which is implicated in metabolic disor...

Insulin resistance is a complex altered metabolic condition characterized by impaired insulin signaling and implicated in the pathogenesis of serious human diseases, such as diabetes, obesity, neurodegenerative pathologies. In pursuing our aim to identify new agents able to improve cellular insu...

The enantioselective conjugate addition of Schiff base ester derivatives to Michael acceptors either in solution (56–89% e.e.) or on solid-phase (34–82% e.e.) gave optically active unnatural α-amino acid derivatives. The reaction was conducted in the presence of chiral, non-racemic quaternary...

(E)-1-{4-[2-(1H-Indazol-3-yl)vinyl]benzoyl}piperazine (KW-2449) is a novel multikinase inhibitor. During our clinical study, we found that KW-2449 is mainly metabolized to its oxo-piperazine form (M1). An inhibition study suggested that monoamine oxidase-B (MAO-B) oxidizes KW-2449 to an iminium ...

A series of metal and amine salts of p-aminosalicylic acid (PAS) were synthesized and their water solubilities and intrinsic dissolution rates investigated. Whilst the increased solubility of PAS in the presence of its major breakdown product m-aminophenol (MAP) dictated that equilibrium solubil...

Three types of petroleum-based tricycloalkyl-containing methacrylate polymers derived from adamantane and DCPD were synthesized and characterized, poly(1-adamantyl methacrylate) (PADMA), poly(tricyclodecyl methacrylate) (PTCDMA) and poly(1-adamantyl methacrylate-co-tricyclodecyl methacrylate) (P...

In this paper, the medium chain glycerides of coconut oil were used as solvolysis reagents for microwave-enhanced conversion of polycarbonate into recycled polyols. First, triglycerides of coconut oil were transesterified with glycerol to monoglycerides bearing functional hydroxyl groups, which ...

The structural, electronic, vibrational and thermodynamic calculations were performed on one of the transition metal dichalcogenides such as molybdenum disulphide named bulk 2H-MoS2, single layer 2H-MoS2 and 3R-MoS2 systems. The dispersion corrected density functional theory (DFT-D) has been emp...

We present the first calculation of piezoelectric constants of 3R-MoS2 which is one of three known polytypes of MoS2. We demonstrate that the 3R-MoS2 structure with 5 layers has the highest reported piezoelectric constant of all MoS2 multilayer structures. The maximum piezoelectric constant is a...

A series of novel 2-(4-(1H-tetrazol-5-yl)-1H-pyrazol-1-yl)-4-(4-phenyl)thiazole derivatives, 6(a–o) were designed, synthesized and evaluated for inhibitory activity against human PDE3A and PDE3B. In PDE3 assay, entire set of targeted analogs showed considerable inhibition of PDE3A (IC50 = 0.24 ...

A mathematical model previously developed to test the validity of categorisation of skin test responders has been applied to data obtained from 3 age groups of Kuwaiti school children. Two specially designed sets of 4 new tuberculins were tested on senior school children to determine whether ext...

A multiple skin test survey of school children (aged 5–15 years) living in Agra, India showed very high levels of sensitisation to numerous species of mycobacteria and little difference in tuberculin positivity between those with and without BCG scars.A total of 136 children aged 3 months to 8 ...

The synthesis of three 1-(4-trifluoromethylphenyl)-3-methyl-4-R1(CO)-5-pyrazolone proligands LH (L1H; R1=C6H5: L2H; R1=CH3: L3H; R1=CF3) and their interaction with R3Sn(IV) acceptors (R=Me, Bun, Ph) are reported. When R=Me or Bun, aquo (4-acylpyrazolonate)SnR3(H2O) derivatives are obtained and...