A novel series of potent C-6 substituted pyrazolo[1,5-a]pyridine inhibitors of herpes simplex viruses has been identified. A synthetic methodology was developed involving functionalization of a C-6 trifluoromethyl pyrazolo[1,5-a]pyridine to allow facile access to a diverse set of analogues from ...

We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly pote...

The reactions of 3-substituted 5-aminopyrazoles with arylidenepyruvic acids and their synthetic precursors, pyruvic acid and aromatic aldehydes, were studied. Several different reaction pathways for these cyclocondensation reactions were established depending on the reaction conditions and build...

Three-component reactions of 5-aminopyrazoles and salicylic aldehydes with pyruvic acids were studied. The method of tuning of the selectivity of the heterocyclizations allowing to change its direction by variation of the reaction parameters was worked out. The treatment involving pyruvic acid c...

5-Methylpyrazole derivative 1 is metallated at the C-5 methyl carbon atom to form lithium 5-lithiomethyl-3-methylpyrazole-1-carboxylate 3 which on reaction with α-oxoketene dithioacetals 4a-d, 12a-c and 15a-b yields substituted and annelated pyrazolo[1,5-a]pyridines 7a-d, 13a-c and 16a-b.

Biological activities of estrogen molecules are altered by fluorination of ring A, and the resulting impairment to form catechols. 2-fluoroestradiol (2-F-E2) has been found to be devoid of carcinogenic action despite its high estrogenic potency; its metabolic effects are so far unknown. This stu...

A new, short synthetic route to 2-fluoroestradiol from 19-nortestosterone is described which gives the target compound in an approximately 25% overall yield. Oxidative defluorination of 2-fluoroestradiol to 2-hydroxyestradiol via treatment with Frémy's salt/iodide ion is reported. This pro...

Two cases of keratitis in patients using ' Exolan ' (triacetoxyanthracene) paste are reported. Although both healed completely with no adverse effects, the severity of the initial lesion implies that this could be a potentially dangerous drug to the cornea.

Both enantiomers of trans-2-phenylcyclohexanol (3), Whitesell's auxiliary, have been prepared in a simple two step sequence featuring a catalytic asymmetric dihydroxylation followed by stereoselective hydrogenolysis

The exploitation of oil sands has raised major environmental concerns, particularly regarding the presence of high concentration in contaminants such as polycyclic aromatic hydrocarbons (PAHs) and naphthenic acids (NAs) in oil sands process-affected water (OSPW). The purpose of this study was, f...

In this study, immobilization of invertase was achieved on a conducting polymer of 1-(4-nitrophenyl)-2,5-di(2-thienyl)-1H-pyrrole) (SNS (NO2)) via electrochemical polymerization. Kinetic parameters, maximum reaction rate (Vmax) and substrate affinity (Km), optimum temperature and pH, operational...

We are continuing our concerted effort to optimize our first lead entry antagonist, NBD-11021, which targets the Phe43 cavity of the HIV-1 envelope glycoprotein gp120, to improve antiviral potency and ADMET properties. In this report, we present a structure-based approach that helped us to gener...

Potassium nitrate is supported on calcined hydrotalcite by a wet mixing method to produce strong basic sites. X-ray powder diffraction patterns reveal that dropping of potassium salt on calcined hydrotalcite promotes the recovery of the layer structure on rehydration. Potassium species are dispe...

Isotactic homopolymers of high optical purity (S)-5-methyl-1-heptene and of 1-heptene have been prepared and studied by 13C n.m.r. The tacticity degree evaluation of the polymers was performed on the basis of skeletal methine or methylene carbon atoms resonances in terms of diads. Conformational...

Ethyl 5-telluro-(2E,4Z)-pentadienoate 2, which is prepared by the Wittig olefination of (Z)-β-telluroacrolein 1, reacted very rapidly with organocuprates 3 at −78°C to form exclusively the corresponding 5-substituted products 4 with high stereoselectivity and in excellent yields.

Methods are described for the preparation of volatile derivatives of amino acids, which permits analysis by gas chromatography. Alanine, glycine, isoleucine, leucine, serine, threonine and valine were converted to the trifluoroacetyl amino acid n-amyl esters, and the separation of these seven co...

N-Acylglycines (NAGs), the endogenous single-tailed lipids present in rat brain and other mammalian tissues, play significant roles in cell physiology and exhibit interesting pharmacological properties. In the present study, a homologous series of N-acylglycine alkyl esters (NAGEs) with matched ...

Due to the ease of processing and stability during filtration, polydopamine (PD) coatings with grafted hydrophilic polymers have recently received significant attention. In this study, glycine-functionalized PVA was synthesized and grafted to a PD-coated ultrafiltration (UF) membrane to improve ...

A catanionic liposomal system made up of lauryl glycinate hydrochloride (LG·HCl) and sodium dodecyl sulfate (SDS) has been characterized by physicochemical techniques. Results of turbidimetric and isothermal titration calorimetric studies gave strong evidence the formation of an equimolar compl...

A series of three new boron-dipyrromethenes bringing different functionalized triphenylamine donor Bodipy–TPA–R (R = BI, BH–OH, BH–COOH) (1–3) together with the reference compound Bodipy–TPA (0), have been synthesized and structurally characterized. Due to their same less electronic coupli...