A series of 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles were efficiently synthesized by oxidative cyclisation of N′-benzylidene-(1H-indol-3-yl)alkane hydrazides using di(acetoxy)iodobenzene. N′-Benzylidene-(1H-indol-3-yl)alkane hydrazides themselves were derived from simple indo...

The chief purpose of this work was to synthesise and find out the anti-oxidant and anti-microbial activities of novel 3-(2-substituted)-1H-indol-3-yl)-1-(thiophen-2yl)prop-2-en-1-one chalcone derivatives. These derivatives were prepared by performing Claisen–Schmidt condensation reaction of 1-(...

A new class of PDE4 inhibitors were designed and synthesized via the InCl3 mediated heteroarylation of indoles and their further derivatization through the Pd(II)-catalyzed CH activation strategy. This effort allowed us to discover a series of 2-(1H-indol-3-yl)-quinoxaline based inhibitors posse...

The HIV-1 Reverse Transcriptase (RT) is a validated and deeply explored biological target for the treatment of AIDS. However, only drugs targeting the RT-associated DNA polymerase (DP) function have been approved for clinical use. We designed and synthesised a new generation of HIV-1 RT inhibito...

2-Oxo-4-(2′-phenyl-5′-substituted 1H-indol-3′-yl)-6-phenylpyridin-3-carbnitriles (2a–c) and its derivatives containing 1,2,4-triazole (4a–c), thiazolo[3,2-b][1,2,4]triazole (5a–c), hydrazide (6a–c), pyrazolones (7a–c) and (8a–c) were synthesized. Structures of all these previously unkno...

The corrosion inhibition potentials of some derivatives of 2-((1H-indol-2-yl)thio)-6-amino-4-phenylpyridine-3,5-dicarbonitrile (TAPD) namely 2-(1H-indol-2-ylthio)-6-amino-4-(4-nitrophenyl)pyridine-3,5-dicarbonitrile (TAPD-I), 2-((1H-indol-2-yl)thio)-6-amino-4-phenylpyridine-3,5-dicarbonitrile (T...

An efficient method for preparation of substituted 6H-isoindolo[2,1-a]indol-6-ones (2) that are important structural components of a vast array of naturally occurring and pharmacologically active compounds, has been developed by the palladium-catalyzed intramolecular cycloaminocarbonylation of 2...

Gastrin-releasing peptide receptors (GRP-Rs, also known as bombesin 2 receptors) are overexpressed in a variety of human cancers, including prostate cancer, and therefore they represent a promising target for in vivo imaging of tumors using positron emission tomography (PET). Structural modifica...

We have previously shown that SMP-304, a serotonin uptake inhibitor with weak 5-HT1A partial agonistic activity, may act under high serotonin levels as a 5-HT1A antagonist that improves the onset of paroxetine in the rat swimming test. However, SMP-304 is mostly metabolized by CYP2D6, indicating...

A mild and efficient copper-catalyzed oxidative trifluoroethoxylation of aryl and heteroaryl boronic acids with CF3CH2OH has been developed. This protocol tolerates a range of functional groups, allowing access to a variety of aryl and heteroaryl trifluoroethyl ethers.

The iminodiacetic acid and aminodiethanol moieties are known for their ability to generate with boronic acids bicyclic structures having a strong intramolecular NB coordination. We describe here the convergent synthesis of 3′-deoxy-3′-iminodiacetic acid and 3′-deoxy-3′-aminodiethanol thymidi...

A new phthalonitrile precursor with tyrosine substituent and the zinc phthalocyanine derived from it were synthesized and their interaction with diphenylborinic acid was studied. The new compounds were characterized by using elemental analysis, IR, 1H and 11B-NMR and UV-VIS spectral data. 11B-NM...

Tamiflu readily undergoes endogenous hydrolysis to give oseltamivir carboxylic acid (OC) as the active anti-influenza agent to inhibit the viral neuraminidase (NA). GOC is derived from OC by replacing the 5-amino group with a guanidino group. In this study, OC and GOC congeners with the carboxyl...

The original synthesis of 6-deoxy-6-fluoro-D-glucose, which involves as the key stage a fluoride-displacement reaction on 3,5-O-benzylidene-1,2-O-isopropylidene-6-O-mesyl-α-D-glucofuranose, has been improved. Treatment of methyl 6-O-tosyl-α-D-glucopyranoside with potassium fluoride in boiling ...

This paper presents both an experimental and theoretical investigation of the consumed and accumulated rates of sulfate ions in concrete. The authors analyze the effects of sulfate solution concentration and the water-cement ratio on the sulfate ions distribution. Based on the diffusion theory, ...

Sulfate and methane diffuse vertically along opposed concentration gradients into the sulfate-methane transition in subsurface marine sediments where anaerobic oxidation of methane with sulfate takes place. The stoichiometry of this process is 1:1, yet the calculated sulfate flux often exceeds t...

During the process of preparing furfural by straw depolymerization with dilute sulfuric acid, large amounts of high temperature sulfate-rich organic wastewater were produced. It cannot be treated directly by anaerobic digestion and converted to bioenergy due to high concentrations of sulfate. In...

A selective and sensitive liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed for the quantitative determination of 1-(3-chloropropyl)-4-(3-chlorophenyl)piperazine HCl (CCP HCl) a process related impurity in trazodone. The method provided excellent sensitivity at a t...

Treatment of arylmethylideneamines with 5-chloropentanoyl chloride in benzene in the presence of 2,6-lutidine afforded novel trans-4-aryl-3-(3-chloropropyl)azetidin-2-ones in good yields. The latter 3-(3-chloropropyl)-β-lactams were transformed selectively into trans-methyl 1-alkyl-2-arylpiperi...

In order to clarify the effect of polar group modification on flotation performance of amine collector, flotation properties of quartz and hematite using bis(2-hydroxy-3-chloropropyl) dodecylamine (N23) as a collector were investigated. And the adsorption mechanism of N23 on quartz surface was e...