Over-activation of N-methyl-d-aspartate (NMDA) receptors is critically involved in many neurological conditions, thus there has been considerable interest in developing NMDA receptor antagonists. We have recently identified a series of naphthoic and phenanthroic acid compounds that allostericall...

Seven novel multicomponent crystals involving various substituted organic amine molecules and 6-hydroxy-2-naphthoic acid were prepared and characterized by using single crystal X-ray diffraction, infrared and thermogravimetric analyses (TGA). Crystal structures with 1,4-bis(imidazol) butane (L1)...

Two new methods for the synthesis of 6-amino-2-naphthoic acid have been described. One of these, i. e., by way of 6-bromo-2-naphthylamine, produces the compound conveniently and in satisfactory quantities. The other method, i. e., by way of 6-nitro-2-naphthylamine, provides a procedure easily ca...

Quaternary phosphonium ion-pair or a salt derived from amino acid has been developed to catalyze the Mannich-type reaction of α-substituted ethyl cyanoacetates and 2-(2-nitrophenyl) acetonitrile to N-Boc imines. Experiments shown that more active cyanoacetates could be catalyzed by the gentle p...

A combination of an amino-acid derived chiral phosphine catalyst and methyl acrylate has been employed to catalyze the direct Mannich reaction of α-aryl isocyanoacetate and N-Boc-aldimines efficiently. The loading of the catalyst could be as low as 0.5 mol% without compromise on the yield and e...

Daphnia magna heartbeat is myogenic—originating within the animal's heart. However, the mechanism for this myogenic automaticity is unknown. The mechanism underlying the automaticity of vertebrate myogenic hearts involves cells (pacemaker cells), which have a distinct set of ion channels t...

Rosin-based resins are utilised commercially in printing ink, adhesive and coating applications. They may incorporate polyhydric alcohols and polybasic acids and are often modified with phenolformaldehyde resins. The composition of tert-butylphenol and p-nonylphenolformaldehyde condensates and t...

The extension of the deprotection procedure of t-butylated carboxyl function using HNO3 in CH2Cl2 to a number of appropriately selected N-Z-derivatives of natural amino acid esters was investigated. The method was found to work effectively with alanine, phenylalanine, serine and the dipeptide as...

β-3-Furylalanine has been synthesized and has been found to inhibit the growth of Escherichia coli, ATCC strain 9723; Escherichia coli, ATCC strain 9723f; and Lactobacillus arabinosus 17-5. In each strain of E. coli, in the presence of exogenous phenylalanine, β-3-furylalanine was more toxic t...

2-(4-Methoxyphenyl)ethyl-2-acetamido-2-deoxy-β-d-pyranoside (salidroside analog-4g, SalA-4g), has shown neuroprotective prospects for the treatment of ischemic stroke. However, the dose–response and time window study for SalA-4g, and the mechanism of SalA-4g-mediated neuroprotection remain unc...

Changes in AMP-activated protein kinase (AMPK) activity contribute to the regulation of insulin secretion. Troglitazone has been shown to lower serum insulin levels and protect beta cell function. The aim of the present study was to examine the effects of troglitazone on AMPK activity and insuli...

Drug-induced hepatotoxicity is a major reason for withdrawal of drugs from development as well as from the market. A major problem predicting hepatotoxicity is the lack of suitable predictive in vitro system. Drug-induced hepatotoxicity is usually associated with the recruitment of immune cells ...

Troglitazone is a thiazolidinedione antidiabetic agent with insulin-sensitizing activities that was withdrawn from the market in 2000 due to its association with idiosyncratic hepatotoxicity. To address the suspected autoantibody production associated with troglitazone, we investigated autoantib...

BackgroundIt has been recognized that insulin hypersecretion can lead to the development of insulin resistance and type 2 diabetes mellitus. There is substantial evidence demonstrating that thiazolidinediones are able to delay and prevent the progression of pancreatic β-cell dysfunction. Howeve...

Troglitazone is a thiazolidinedione insulin sensitizer drug for the treatment of type 2 non-insulin-dependent diabetes mellitus (NIDDM). Based on an increasing number of reports on troglitazone-associated liver toxicity, the cholestatic potential of troglitazone and its major metabolite troglita...

Rp and Sp diastereomers of the 5′-dimethoxytrityl-2′-deoxynucleoside-3′-Omethylphosphonamidites of N6-Benzoyl-adenine, N2-isobutyryl-guanine, N4-benzoylcytosine, and thymine were separated by liquid chromatography on a normal phase silica column eluted with 1.0% EtOH in CHCl3.

Novel stereoisomeric natural pinane-derived bifunctional catalysts 3a–d bearing a pyrrolidine unit have been synthesized and examined in the asymmetric conjugate additions of carbonyl compounds to α-nitroalkenes. Six-membered cyclic ketones react with β-nitrostyrene derivatives in the presenc...

SummaryWe present a molecular modeling and simulation study of the E. coli cell envelope, with a particular focus on the role of TolR, a native protein of the E. coli inner membrane, in interactions with the cell wall. TolR has been proposed to bind to peptidoglycan, but the only structure of th...

The tolQ, R, A and B genes have been isolated from the DNA of Haemophilus influenzae and sequenced. The deduced amino acid (aa) sequence of the H. influenzae TolQ, ToIR, TolA and TolB show 67, 63, 41 and 62% identity with Escherichia coli TolQRAB proteins, respectively. These four proteins are i...

Edwardsiella ictaluri is a Gram-negative intracellular facultative pathogen causing enteric septicemia of channel catfish (ESC). The Tol system, consisting of four envelope proteins TolQ, TolR, TolA, and TolB, are required for colicin import and contributes to bacterial virulence in several path...