trans-β-Bromostyrenes have been conveniently prepared in moderate to high yield in a one-pot two-step sequence.trans-1,2-Bis(tri-n-butylstannyl)ethylene underwent a smooth palladium(0) catalyzed coupling reaction with 0.5 equivalents of aromatic bromide or iodide to furnish atrans-β-stannylsty...

An efficient and one-step versatile method for the synthesis of benzimidazoles and 1H-imidazo[4,5-b]pyridines from quinoxalinones and their aza-analogues have been developed on the basis of the novel ring contractions of 3-aroyl-quinoxalinones and their aza-analogues with 1,2-arylenediamines.

A series of 4-alkylaminoaryl phenyl cyclopropyl methanones (6a–6u and 8a–8c) were synthesized from 4-fluorochalcones (3a and 3b) by cyclopropanation of double bond followed by nucleophilic substitution of F with different amines. The compounds were screened for their antitubercular and antimal...

SIRT1 is a NAD+-dependent deacetylase. Here we described new SIRT1 inhibitors with the scaffold of benzofuran-3-yl(phenyl)methanone. The inhibitors were predicted to bind in C-pocket of SIRT1, forming hydrophobic interactions with Phe273, Phe312 and Ile347. Introducing hydroxyl to meta position ...

An efficient method for the synthesis of 1-chlorophenazines has been established. It is based on the use of 3,6,6-trichloro-2-hydroxy-2-cyclohexen-1-one 4 as a synthetic equivalent of 3-chloro-1,2-benzoquinone 3. The intermediate 4 was prepared in near quantitative yield by electroreductive mono...

Synthesis of a new photolabile protecting group, bis(4,5-dimethoxy-2-nitrophenyl)ethylene glycol (4) from 4,5-dimethoxy-2-nitrobenzyl alcohol in three steps in good yields is described. The acetals and ketals of 4 are stable against acidic and basic reaction conditions and are cleaved smoothly o...

Ultraviolet(UV)-induced photodeprotection of 2-nitrobenzyl esters to release the acid with formation of the corresponding 2-nitrosoketone proceeds rapidly when the α-position in the 2-nitrobenzyl group is substituted by a branched alkyl group. The generated 2-nitrosophenyl ketones undergo multi...

We now describe the preparation and characterization of a novel radioligand, 2-[125I]]iodo-5-methoxy-carbonylamino-N-acetyltryptamine (2-[125I]MCA-NAT), with high affinity and pharmacological selectivity for melatonin ML2 receptor sites. 2-[125I]MCA-NAT was prepared by introducing an [125I]iodin...

Several studies have implicated the suprachiasmatic nuclei (SCN) as a target for the action of melatonin in its regulation of seasonal and circadian behaviour. Single-unit activity from the SCN and adjacent paraventricular area and anterior hypothalamus was recorded using the in vitro rat hypoth...

A sensitive, rapid, and economical method has been developed for determination of serotonin N-acetyltransferase activity from a variety of enzyme sources. The assay is based upon separation and detection of N-acetyltryptamine formed from tryptamine and acetyl coenzyme A, by means of high-perform...

Enantioselective synthesis of C23–C28 subunit of campestane steroids based on catalytic methods is reported. The synthesis was started from (S)-2-isopropyl-4-nitrobutan-1-ol, which is easily accessible by the reaction between isovaleraldehyde and nitroethylene catalyzed by only 2% of (S)-trimet...

We report new examples of a series of losartan–hydrocaffeic hybrids that bear novel ester, amide and amine linkers. These compounds were made by linking hydrocaffeic acid to the side chain of losartan at the C-5 position of the imidazole ring through different strategies. Experiments performed ...

A practical synthesis of (2R,3S)- and (2S,3R)-β-methyltryptophan ethyl ester (β-MeTrp-OEt) has been developed. Racemic threo-β-MeTrp-OEt was diastereoselectively prepared via crystallization-induced diastereomer transformation (CIDT) of the α-nitro equivalent of β-MeTrp-OEt. The enantiomers...

A series of novel substituted 2-(phenyl)-3H-benzo[d]imidazole-5-carboxylic acids (1a–1j) and its methyl esters (2a–2f) were synthesized and examined for their antiproliferative effects against three breast cancer cell lines (MDA-MB231, MDA-MB468 and MCF7) in vitro. Most of the compounds exhibi...

Ethylhexyl methoxy cinnamate (EHMC) is one of the major organic ultraviolet (UV) filter pollutants in the environment. The purpose of this study was to investigate the parental transfer of EHMC and induced biochemical responses in zebrafish (Danio rerio). Zebrafish embryos were exposed to EHMC so...

The interactions between sulfur-containing compounds of dibenzothiophene (DBT) and dibenzothiophene sulfone (DBTO2) and ionic liquids of 1-butyl-3-methylimidazolium hexafluorophosphate ([BMIM]+[PF6]−) and 1-butyl-3-methylimidazolium tetrafluoroborate ([BMIM]+[BF4]−) were comparatively studied by...

The oxidation of dibenzothiophene (DBT) to dibenzothiophene-sulfone (DBT-sulfone) has been a topic of particular interest in the past few years, as a possible technique to remove sulfur from crude oil. In this manuscript we show that the oxidation of DBT to DBT-sulfone occurs using silica and do...

Dibenzothiophene sulfone (DBTO) adsorption utilizing clay material adsorbents such as activated clay, bentonite and kaolinite were investigated in this study. The properties of each adsorbent were characterized using Fourier transform infrared spectroscopy, scanning electron microscope, Brunauer...

Syntheses and spectroscopic characterization data for two new hybrid chelating ligands, 4,6-bis[(diphenyl-N,N-diethylcarbamoylmethylphosphine oxide)methyl]dibenzothiophene (2) and 4,6-bis[(diphenyl-N,N-diethylcarbamoylmethylphosphine oxide)methyl]dibenzothiophene 5,5-dioxide (3), that contain tw...

Biodesulfurization is an eco-friendly process for removing sulfur from petroleum fractions. The process could not be commercialized because of the inability of microorganisms to desulfurize a wide range of heterocyclic poly aromatic sulfur compounds like dibenzothiophene (DBT), 4, 6-Dimethyl DBT...