The divergent syntheses of the trichloroacetamide derivatives of (2S,3R,8R,9R,4E,6E)-3-amino-9-methoxy-2,6,8-trimethyl-10-phenyl-decadenoic acid (enantio-iso-ADDA), and (2R,3R,8R,9R,4E,6E)-3-amino-9-methoxy-2,6,8-trimethyl-10-phenyl-decadenoic acid (enantio-ADDA), have been achieved. Our approac...

Diastereoselective alkylation of (R)-(+)-camphor-based glycine or alanine esterimines with 3-bromo-2-fluoropropene after hydrolytic deprotection gave (R)-(+)-2-amino-4-fluoropent-4-enoic acid with 38% overall yield and 90% ee, or (R)-(+)-2-amino-4-fluoro-2-methylpent-4-enoic acid (19% overall yi...

Triflic acid-mediated stereoselective direct lactonization of a variety of α-amino γ,δ-unsaturated carboxylic acid esters and the construction of new γ-butyrolactone structural motifs are reported. Several α-amino γ,δ-unsaturated carboxylic acid esters underwent stereo- and regioselective...

A convenient synthesis of δ,γ-unsaturated amino acids has been developed. After a mixture of (R)-tert-butanesulfinamide and glyoxylic acid with molecular sieves in CH2Cl2 was stirred for 42 h at room temperature, allylboronic acid pinacol ester was added to the mixture to give (R)-2-((R)-tert-...

Amino-bisphosphonates (alendronate, pamidronate) were covalently linked in a three step synthesis, with protected and triazolylated derivatives of therapeutically used nucleoside analogs (5-FdU, araC, AZT) by substitution of their triazolyl residue. From the deprotected and chromatographically p...

The preparation, crystal structures and magnetic properties of two complexes containing bis(maleonitriledithiolate)nickel(III)/copper(II) anion, [4BrBzTPP][Ni(mnt)2] (1) and [4BrBzTPP]2[Cu(mnt)2] (2) ([4BrBzTPP]+ = 1-(4′-bromobenzyl)triphenylphosphinium) are report here. The crystals of two com...

Photophysical properties of (E)-1-(4-bromobenzyl)-4-(4-hydroxy-3-methoxystyryl) pyridinium bromide existing in equilibrium of its protonated (BSHB) and deprotonated (BS) forms at different pH were characterized by UV–Vis spectroscopy, and steady-state, and time-resolved fluorescence techniques....

Base-induced cycloaddition of ethyl isocyanoacetates to trifluoroacetimidoyl chlorides gives ethyl 5-trifluoromethylimidazole-4-carboxylates with high regioselectivity.

A series of four N-benzylamides of γ-hydroxybutyric acid (GHB), that contain N-(4-phenylpiperazine)-, N-(4-benzylpiperazine)rings, N-benzylamino-, or N-(2-phenylethylamine)-groups in the α-position of GHB were selected as model compounds, for determining the structural elements responsible for...

BackgroundEGb-761 is an antioxidant and anticarcinogen; however, its role as a photoprotector remains unknown.

Extracts from leaves of Ginkgo biloba are among the most widely used and best investigated phytopharmaceuticals worldwide. Almost all clinical trials and the majority of preclinical studies have been performed with a specifically defined extract (EGb 761®) standardized to contain confined concen...

Mitochondria are dynamic organelles that constantly undergo fission and fusion. The balance between fission and fusion determines the fate of the cell. In this study, we show that mitochondrial fission factor (MFF) is upregulated upon hydrogen peroxide treatment or ischemia/reperfusion (I/R) inj...

Ginkgo biloba has been used in herbal medicines for thousands of years. Although a standard G. biloba extract, EGb 761 has been used to improve cognition in breast cancer patients, its effects on breast cancer are unknown. Therefore, we investigated the antitumorigenic effects of EGb 761 using a...

EGb 761 is a standardized natural extract from Ginkgo biloba leaf that has shown neuroprotective effects after ischemic stroke. This study aimed to use magnetic resonance imaging (MRI) to noninvasively evaluate whether EGb 761 promotes neurovascular restoration and axonal remodeling in a rat mod...

IntroductionTinnitus is defined as the perception of sound without its actual presence in the environment. It has been the subject of a great number of studies, especially considering its consequences on patient’s quality of life.

(E)-(4-(2-(benzo[d]thiazol-2-yl)hydrazono)-3-methyl-2,6-diphenylpiperidin-1-yl)(phenyl)methanone [EPHDPM] and its derivatives were synthesized and characterized by FT-IR, 1H NMR, 13C NMR and elemental analysis. The target compound [EPHDPM] was computed using density functional theory (DFT) metho...

Mono(iminophosphorane) 4 was selectively prepared from the reaction of 3,4-diaminothieno[2,3-b]thiophene 3 with excess triphenylphosphine, C2Cl6, and Et3N due to intramolecular double hydrogen bond formation. Mono(iminophosphorane) 4 reacted with aromatic isocyanates to give stable carbodiimides...

In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound class is phototoxic in vitro. Here we describe a n...

The nickel-phosphate decorated phosphate-Fe2O3 photoanode (NiPi/Pi-Fe2O3) was fabricated by coating phosphate modified hematite (Pi-Fe2O3) with naturally abundant nickel-phosphate complexes (NiPi). X-ray powder diffraction, scanning electron microscopy, transmission electron microscopy and energ...

SummaryA well documented study on the anticonvulsant properties of 4-amino-N-(2-ethylphenyl)benzamide (4-AEPB) is here provided. Initial screening in mice dosed intraperitoneally and rats dosed orally indicated that 4-AEPB is active against maximal electroshock—induced seizures (MES), but does ...