The corrosion inhibition efficiency of 3,7-dimethyl-1-(prop-2-yn-1-yl)quinoxalin-2(1H)-one (DPQO) on carbon steel in 1.0 M HCl solution has been investigated using, potentiodynamic polarization, electrochemical impedance spectroscopy (EIS), weight loss, and scanning electron microscopy (SEM) met...

The palladium-catalyzed direct alkynylation of 2,2-difluoro-1-tributylstannylethenyl p-toluenesulfonate 1 with alkynyl bromides provided the corresponding 1,1-difluoro-1,3-enynyl tosylates 2 in good yields. The Suzuki-Miyaura arylation reaction of 2 with arylboronic acids afforded the cross-coup...

MicroRNA-21, as an oncogenic miRNA, has caught great attention for medicinal chemists to develop its novel inhibitors for cancer therapy. In the present study, we designed 4-benzoylamino-N-(prop-2-yn-1-yl)benzamides as miR-21 inhibitor candidates on the basis of scaffold hopping. Eighteen compou...

A new series of 2,6-diaryl-1-(prop-2-yn-1-yl)piperidin-4-one oximes (17–24) were designed and synthesized from 2,6-diarylpiperidin-4-one oximes (9–16) with propargyl bromide. Unambiguous structural elucidation has been carried out by investigating IR, NMR (1H, 13C, 1H−1H COSY and HSQC), mass s...

2-Methylquinoline reacts with 1-(het)aryl-3-phenylprop-2-yn-1-ones under mild transition metal-free conditions (55–60 °C, 20 mol% KOH, H2O, MeCN) to afford 2-{5’-(het)aryl[1,1’ : 3’,1”]terphenyl-4’-yl}quinolines in up to 35% yield. The reaction likely proceeds via the intermediate 1,3-dip...

In this work, we described a new synthetic route of 3-bromo-1,2-dihydroquinoline derivatives based on the TBAB/Oxone-mediated radical 6-endo-trig ortho-cyclization of 2-alkynylbenzamide. The reaction proceeded smoothly with moderate functional group tolerance and high reaction efficiency. It is ...

This work describes the copper-catalyzed Csp-chalcogen bond formation through cross-coupling reactions of propynylbenzamides and diorganyl dichalcogenides at room temperature, under open atmosphere. Generally, the reactions have proceeded very smoothly, affording the new class of organochalcogen...

The synthesis and utility of β-oxotryptamine and β-oxytryptophan ester synthons provide a convenient entry to 5-(3-indolyl)oxazole natural products leading to a structure revision of almazole D.

4,4-Dimethyl-2-(3-chloro-2-methyl-1-propenyl)-2-oxazoline has been synthesized and deprotonated with LDA in THF to give the corresponding lithiated species, which has been found to react α-regioselectively with NH4Cl and alkyl halides, and γ-regioselectively with carbonyl compounds to afford α...

Three new compounds, identified as (3S)-5-hydroxy-3-(2-hydroxybenzyl)-7-methoxychroman-4-one, oleracone C (1), 5-hydroxy-3-(2-hydroxybenzyl)-7-methoxy-4H-chromen-4-one, oleracone D (2), and 1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(2-hydroxyphenyl)propan-1-one, oleracone E (4), together with one new ...

The physiological importance of reactive sulfur species (RSS) such as cysteine hydropersulfide (CysSSH) has been increasingly recognized in recent years. We have established a reactive sulfur metabolomics analysis by using RSS metabolic profiling, which revealed appreciable amounts of RSS genera...

Bazedoxifene is a selective estrogen receptor modulator (SERM) that has been developed for use in post-menopausal osteoporosis. However, it contains a potentially toxic 5-hydroxy-3-methylindole moiety. Previous studies on the 5-hydroxyindole and the 3-alkylindole-containing drugs indometacine, z...

A series of 6-aminonicotinic acid analogues have been synthesized and pharmacologically characterized at native and selected recombinant GABAA receptors. 6-Aminonicotinic acid (3) as well as 2- and 4-alkylated analogues (9–11, 14–16) display low to mid-micromolar GABAAR binding affinities to n...

Compared to most normal cells that express L-type amino acid transporter 2, L-type amino acid transporter 1 is highly expressed in cancer cells and presumed to support their elevated growth and proliferation. This study examined JPH203, a potent and selective L-type amino acid transporter 1 inhi...

The fluorescence properties of the aflatoxins M1, Q1, P1 in solution and the effect of various cyclodextrins (α-, β-, γ-, hydroxypropyl-β- and α-β-heptakis-di-O-methyl-β-) on their fluorescence emission were studied. Among the aflatoxins, a substantial enhancement of the fluorescence emis...

SummaryPatients infected with hepatitis C virus (HCV) have an increased risk of developing type 2 diabetes. HCV infection is linked to various liver abnormalities, potentially contributing to this association. We show that HCV infection increases the levels of hepatic selenoprotein P (SeP) mRNA ...

Quinacridone stands out among many optical materials, because it possesses a large π-conjugated system, remarkable photothermal stability, excellent semiconductor property, and easy modification at multiple active sites of parent molecule. In this paper, the functionalized D-A poly-quinacridone...

In the present work, the temperature dependences of heat capacities of block copolymers of chitosan with poly(D,L-lactide) have been measured in the temperature range from 6 to 350 K by precision adiabatic vacuum calorimetry, and thermophysical properties of copolymers have been studied over the...

Fermentation of optically pure D-lactic acid was carried out using cassava starch as the main substrate. For downstream processing, membrane-based processes consisted of microfiltration, nanofiltration, and pervaporation-assisted esterification were successfully employed for the production of hi...

A range of amphiphilic diblock and triblock copolymers based on poly (2-methyl-2-oxazoline) (PMeOx) and poly (D,L-lactide) (PLA) with various compositions and molecular masses were prepared combining cationic ring-opening polymerization and click chemistry. Their hydrophilic weight ratios (f) co...