All-trans-retinoyl chloromethane is a potent irreversible inactivator of bovine opsin in retinal rod outer segments. The inactivation appears to be due to specific modification of the apoprotein at the 11-cis-retinaldehyde binding site. The reaction follows pseudo first order kinetics at 37°C. ...

Tumor metastasis is usually a serious problem in tumor patients because of the lack of therapeutic approaches. A new compound, N-all-trans-retinoyl-l-proline (ATRP), has been developed and its metastasis inhibition activity has been studied. Low concentrations of ATRP have already been found to ...

The optimized molecular structure, vibrational frequencies, corresponding vibrational assignments of 2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone (BHMBC) have been investigated by using density functional theory (B3LYP) methods at 6-311G(d,p) basis set. The energy and oscillator strengt...

Computational and spectroscopic properties of a novel Schiff base compound, 3-hydroxy-4-methoxybenzylidene(2-hydroxyphenyl)amine were studied. The crystal structures of the title compound and its corresponding zwitterionic form were analyzed by X-ray diffraction. The presence of NH, CO and CN st...

A convenient and facile synthesis of t-butyl-2-(4-hydroxy-3-methoxybenzylidene)hydrazine carboxylate (1) was accomplished by refluxing t-butyl carbazate with an appropriate aldehyde in ethanol. The resulting compound was characterized using spectral data analysis augmented by X-ray. Single cryst...

The dehydratases (DHs) of modular polyketide synthases (PKSs) catalyze dehydrations that occur frequently in the biosynthesis of complex polyketides, yet little is known about them structurally or mechanistically. Here, the structure of a DH domain, isolated from the fourth module of the erythro...

Two carbon materials, multi-walled carbon nanotubes (MWCNT) and activated carbon (AC), were investigated as ozonation catalysts for the erythromycin (ERY) mineralization. In addition, in order to evaluate a possible synergetic effect between carbon materials and ceria in the ozonation of this an...

A series of 2-oxy-substituted 1-(1H-imidazol-1-yl)-4-phenylbutanes comprising imidazole–ketones, imidazole–dioxolanes, and imidazole–alcohols substituted with halogens in the phenyl ring were synthesized and evaluated as novel inhibitors of heme oxygenase which are structurally distinct from ...

5-(1-Methyl-4-phenyl-imidazol-5-yl)indoles 5 were prepared and tested as analogs of the natural vascular-disrupting agent combretastatin A-4 (CA-4). The 3-bromo-4,5-dimethoxyphenyl derivative 5c was far more active than CA-4 with low nanomolar IC50 concentrations against multidrug-resistant KB-V...

ABSTRACT. 6-Methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole is a high affinity (Ki = 8.2 nM) reversible inhibitor of acetylcholinesterase (AChE). The carbon-11 labeled form was prepared in high (>97%) radiochemical purity and with specific activities of 37 ± 20 GBq/μmol a...

The reactions of the 1,1′-bis(1-hydroxyalkyl)ferrocenes and 1,1′-bis(1-hydroxy-1-phenylmethyl)ferrocene with thioglycolic acid give the 1,1′-bis[1-(carboxymethyl)thioalkyl]ferrocenes and 1,1′-di[1-(carboxymethyl)thio-1-phenylmethyl]ferrocene which have been characterized by IR and 1H NMR spe...

The aldol condensation of 2-(tert-butyldimethylsilyloxy)-5-methyl-furan 4 with several phenylacetaldehydes led stereoselectively to the syn or the anti aldols under fluoride- or Lewis-acid-promoted conditions. However low yields are obtained due to the formation of the double condensation produc...

A total of 42 benzyl- and pyridylmethyl amines were synthesized either by reductive amination of aromatic/heteroaromatic aldehydes with amines or by conjugate addition of amines to the cinnamates followed by reduction of the ester group with lithium aluminium hydride to the respective propanolam...

The pharmacological properties of the novel ligand, (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol (I), at the human adenosine receptors were investigated using Chinese hamster ovary cell lines recombin...

In this work, rice husk ash (RHA), as a natural source of amorphous silica, was used as a support for the immobilization of 1-methyl-3-(trimethoxysilylpropyl)-imidazolium hydrogen sulfate. The immobilized acidic ionic liquid was characterized with a variety of techniques, including infrared spec...

ZusammenfassungOctadiin-(1,5) isomerisiert bei 425° zu 1-Äthyl-3,4-bismethylen-cyclobuten-(1). Das hieraus durch Addition von Chlorwasserstoff gebildete Isomerengemisch von 3,4-Dichlor-äthyl-dimethylcyclobutenen-(1) bildet in glatter Reaktion mit Dieisenenneacarbonyl d1-Äthyl-2,3-dimethyl-cyclo...

We have previously reported the isolation of four compounds, caffeoyloxy-5,6-dihydro-4-methyl-(2H)-pyran-2-one (CDMP), olinioside, caffeic acid and 3-hydroxylup-12-en-28-oic acid, from the leaves of Olinia usambarensis. Here, we evaluated the inhibitory effects of these compounds on lipopolysacc...

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) represent an integral part of the currently available combination antiretroviral therapy (cART) contributing to reduce the AIDS-mortality and turned the disease from lethal to chronic. In this context we recently reported a series of 6-chl...

2-Alkoxy pyrazino[2,3-e][1,4]diazepin-5-one and 11-alkoxy pyrazino[2,3-e]pyrrolo[1,2-a][1,4]diazepin-5-one derivatives were synthesized via the corresponding iminophosphoranes derived from 3-aminopyrazine-2-carboxylic acid and α-amino acid derivatives, by the intramolecular aza-Wittig methodolo...

A new phosphonate analogue of (+)-porothramycin has been synthesized from (S)-pyroglutaminol. Circular dichroism of diastereomeric intermediates 9 has been studied. The cytostatic activity of the new pyrrolo[2,1-c][1,4]benzodiazepine has been evaluated against human KB cells.