Alterations in serotonin and norepinephrine neuronal functions have been observed in patients with major depression. Several antidepressants bind to both serotonin transporters and norepinephrine transporters (NET). The ability to image NET in the human brain would be a useful step toward unders...

NPY is the most potent orexigenic agent known to man, with NPY Y1 and NPY Y5 being the receptor subtypes that are most likely responsible for centrally-mediated NPY-induced feeding responses. Based on the aforementioned, novel hydrazide derivatives were prepared for the purpose of searching new ...

Phoslactomycins (PLMs) A–F, produced by actinomycetes are polyketide-type antibiotics derived from a hydroxycyclohexanecarboxylic acid or a cyclohexanecarboxylic acid starter unit. Feeding experiments with [2-13C]shikimic acid indicated that the C-18 carbon of PLMs comes from C-5 of shikimate. ...

Previous studies from our laboratory have revealed that esterification/amidation of the carboxylic acid moiety in the nonsteroidal anti-inflammatory drug, indomethacin, generates potent and selective COX-2 inhibitors. In the present study, a series of reverse ester/amide derivatives were synthes...

The role of 5-HT1A and 5-HT2 receptors in mediating foot-shock-induced ultrasonic vocalisation has been studied in rats. Furthermore, behavioural effects were correlated to receptor reserves in the brain by means of receptor inactivation with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)...

Publisher SummaryThe chapter presents a study on quantitation of epoxy- and dihydroxyeicosatrienoic acids by stable isotope-dilution mass spectrometry. The chapter describes a method for measurement of picomolar amounts of epoxyeicosatrienoic acids (EET) and dihydroxyeicosatrienoic acids (DHET) ...

From its microwave rotational spectrum, 6-methyl-3-heptyne (MHept, ethyl isobutyl acetylene) has been characterized in two conformations of Cs and C1 symmetry with the opposing alkyl groups arranged syn-eclipsed or nearly so about the CC axis. The dominant interaction determining the dihedral an...

Repertaxin is a new non-competitive allosteric blocker of interleukin-8 (CXCL8/IL-8) receptors (CXCR1/R2), which by locking CXCR1/R2 in an inactive conformation prevents receptor signaling and human polymorphonuclear leukocyte (PMN) chemotaxis. Given the unique mode of action of repertaxin it wa...

A new hydroxybenzofluorenone has been designed and synthesised in order to investigate the origin of excited state intramolecular proton transfer reactions in this family of compounds. 10-Hydroxy-11H-benzo [b]fluoren-11-one (10-HHBF) does not show dual fluorescence in contrast to its well known ...

Structure-based drug design was utilized to develop novel, 1-hydroxy-2-naphthoate-based small-molecule inhibitors of Mcl-1. Ligand design was driven by exploiting a salt bridge with R263 and interactions with the p2 pocket of the protein. Significantly, target molecules were accessed in just two...

The one-pot reaction of α-, β-alanine with 1-iodopropan-2-one, 2-iodo-1-phenylethanone and 2-iodo-1-(2-thienyl)- ethanone and elemental iodine proceeds without solvents and basic media to afford a novel family of ionic liquids with triiodide counteranion.

The palladium-catalyzed synthesis of unsymmetrical 1,3-diheteroarylbenzenes was investigated. The first synthetic pathway relies on the desymmetrization of benzene-1,3-disulfonyl dichloride through two successive palladium-catalyzed direct desulfitative arylations with two different heteroarenes...

γ-Cyclodextrin having photochromic 1,2-bis(1-benzothiophen-3-yl)perfluorocyclopentene was synthesized. The circular dichroism and the optical rotation of the modified cyclodextrin reversibly changed in aqueous solution by alternate irradiation with UV/visible light.

Photochromism of bis(2-n-alkyl-1-benzothiophen-3-yl)perfluorocyclopentene derivatives has been studied in solution as well as in the single crystalline phase. Introduction of the long alkyl chains at 2-positions of bis(1-benzothiophen-3-yl)perfluorocyclopentene was found to increase the cyclizat...

Highly-thermostable but degradable polyamides have been synthesized by a polycondensation of bio-derived itaconic acid salts with aromatic diamines to form heterocyclic pyrrolidone ring in the polymer backbone. The molecular weight was greater than 33,600 g/mol. Glass transition temperatures, Tg...

The complex (LaL3) of lanthanum (III) with N-(2-amino ethyl) maleamic acid radical (L−) was synthesized and characterized by Fourier infrared spectrum (FT-IR), elemental analysis and melting point measurements. The complex LaL3 was a chelate, in which lanthanum (III) ion was coordinated with the...

The FTIR and FT-Raman spectra of (2S)-2-[(2-{[(2S)-1-hydroxybutan-2-yl]amino}ethyl)amino]butan-1-ol have been recorded in the region 4000–400 cm−1and 4000–100 cm−1 respectively. Utilizing the observed FTIR and FT-Raman data, a complete vibrational assignment and analysis of the fundamental vib...

In this work, a green composite from poly(3-hydroxybutyrate), or P(3HB), grafted with 2-amino-ethyl methacrylate, hydroxylated resin and silica nanoparticles was developed. The goal was to determine if the new poly(urethane-urea) composite can work as an appropriate substrate for biological appl...

This work presents the synthesis of 4-(2-(ethyl(m-tolyl) amino) ethoxy) phthalonitrile (1) as ligand and its peripherally tetrasubstituted metal-free (2) and metallophthalocyanines (3–5) derivatives. Synthesized compounds were characterized by standart spectroscopy methods. The molecular struct...

The mechanisms for the Csp3-H functionalization of ethyl 2-(methyl(p-tolyl)amino)acetate have been investigated using DFT method at the M06-2X/6-31+G(d, p) level, and the SMD model was applied to simulate the solvent effect. The computational results show that the Csp3-H functionalization has fo...