A new series of electroluminescent polymers has been synthesized by incorporating the segments of 2,5-dicyano-1,4-phenylenevinylene (DCN-PV) into the backbone of poly(2-methoxy-5-(2′-ethyl-hexyloxy)-p-phenylene vinylene) (MEH-PPV). The copolymers have similar optical properties with MEH-PPV. Th...

A series of 4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2-naphthalenecarboxamide dopamine (DA) D3 receptor agonists has been identified. These compounds were found to be selective for DA D3 over D2 receptors and were shown to be partial to full agonists as measured by stimulation of mito...

A series of 4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-(substituted benzyl) piperidines with substituents at the ortho and meta positions in the aromatic ring of the N-benzyl side chain were synthesized and their affinities and selectivities for the dopamine transporter (DAT), serotonin transporter...

The serotonin2A (5-HT2A) receptor is implicated in the pathophysiology of schizophrenia and mood disorders, and in vivo studies of this receptor would be of value in studying the pathophysiology of these disorders and in measuring the relationship of clinical response to receptor occupancy for 5...

2-{[3-Cyano-4-(N-ethyl-N-(2-hydroxyethyl)amino)styryl]-5,5-dimethylfuran-2(5H)-ylidene}malononitrile styryl dye was prepared by the condensation of 4-[(2-hydroxy-ethyl)-methyl-amino]-benzaldehyde (donor moiety) with 2-cyanomethylene-3-cyano-4,5,5-trimethyl-2,5-dihydrofuran (acceptor moiety). The...

Base catalysed ring opening ring closure (RORC) reaction of chromone-3-carbonitrile (1) with 2-cyano-N-cyclohexylacetamide afforded 2-amino-N-cyclohexyl-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxamide (ACCP). Mullikan atomic charges and EHOMO-ELUMO highest occupied and lowest unoccupied energies ...

L-alanine methyl ester hydrochloride, 2-aminoisobutyric acid and some condensed 1,4-dihydropyridine derivatives (Compounds R1–R4) were gamma irradiated, the induced free radicals was investigated at room temperature by electron spin resonance techniques. The observed paramagnetic species of ami...

Alpha-aminoisobutyric acid (AIB) labeled with the cyclotron-produced, positron-emitting radionuclide 11C has been synthesized with the label in the alpha-methyl group. Our previously published synthesis of [11C] AIB in the carboxyl position from [11C] HCN requires a rigorous quality assurance pr...

The chiral deuterium- and 13C-isotope-labeled α-aminoisobutyric acids CD3-Aib and 13CH3-Aib were enantioselectively synthesized from L-Ala aldimine using simplified Maruoka chiral phase-transfer catalysts. Homo-chiral (S)-CD3-Aib homopeptides, up to decamers, were prepared. A (R)-CD3-Aib polyme...

Four novel ion-exchangers (Fx-Rt (I), Fx-TPB (II), Cp3-PMA (III) and Cp3-PTA (IV)) of antispasmodic and anticholinergic drugs, flavoxate hydrochloride (FxCl), 2-piperidinoethyl-3-methyl-4-oxo-2-phenyl-4h-1-benzopyran-8-carboxylate hydrochloride, cyclopentolate hydrochloride (CpCl) and (2-(dimeth...

A diastereomeric mixture of racemic α-amino nitriles [1SR,2RS,(SR)]- (1) and [1SR,2RS,(RS)]-N-cyano(phenyl)methyl-1-aminoindan-2-ol (2) was thermally epimerized in the solid state to give diastereopure [1SR,2RS,(SR)]-1. The reaction was about 26 times slower than the same reaction of a mixture ...

Pseudomonas cepacia lipase (PSL) efficiently catalyses the kinetic resolution of (±)-cis- and (±)-trans-1-aminoindan-2-ol through the O-acylation reaction of the corresponding N-benzyloxycarbonyl derivative using vinyl acetate as the acyl donor. In a similar way, cis-N-Cbz-2-aminoindan-1-ol is...

Photodynamic therapy (PDT) is a tool for the treatment of certain cancerous and pre-cancerous conditions in dermatology. 5-Aminolevulinic acid (5-ALA) and simple derivatives thereof are the principal compounds used for this purpose. For optimal efficacy, the drug must be released at an appropria...

In this phase of structure–affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one ...

Folates and folate-like molecules represent a class of vectors for drug targeting and delivery. The folate receptor (FR) is overexpressed in many human cancers, therefore folate-cytotoxic drug conjugates can deliver therapeutic agents specifically to FR positive tumours. We have linked, directly...

A new series of phenanthridinone derivatives, and diketo acid analogs, as well as related phenanthrene and anthracene diketo acids have been synthesized and evaluated as HIV integrase (IN) inhibitors. Several new β-diketo acid analogs with the phenanthridinone scaffold replaced by phenanthrene,...

The mixed ligand copper(II) complex of succinate and 2,2′-bipyridyl was synthesized from disodium succinate, 2,2′-bipyridine and copper nitrate. The structure of the synthesized complex was determined by micro-analysis, IR, thermogravimetric analysis and X-ray crystallography. The thermal deco...

The tris(2,2′-bipyridyl) complexes of cobalt(II) and (III) ([Co(bpy)3]2+/3+) produce a redox couple of great interest in thermoelectrochemical cells and dye sensitized solar cells including both types of devices based on ionic liquid electrolytes. We present a systematic study of the electroche...

A series of anhydrous eight-coordinate air and moisture stable lanthanide (III) complexes of 1,1,1-trifluoro-2,4-pentanedione (tfaa) and 2,2′-bipyridyl (bpy) of the type [Ln(tfaa)3(bpy)] [Ln = La (1), Nd (2), Ho (3), Er (4), Yb (5) and Lu (6)] have been synthesized in high yield by a one-step m...

Tris(2,2′-bipyridyl)ruthenium (II) (Ru(bpy)32+) electrochemiluminescence is one of the most successful electrochemiluminescent systems and has broad range of applications. Most analytical applications of tris(2,2′-bipyridyl)ruthenium (II) electrochemiluminescence involve coreactants. We compre...