Acylimidodicarbonates obtained from aziridine-2-carboxamides through Davidsen bis-Boc activation react with amine nucleophiles under mild conditions to form tertiary aziridine-2-carboxylic acid amides. NH aziridine-2-carboxylic acid amides were obtained by hydrogenolythic deprotection of N-Cbz d...

Isazophos applied as an in-furrow spray at 0·5, 0·75 and 1·0 kg a.i./ha (4·65, 6·98 and 9·3 g a.i./100 m of row) reduced the establishment of Yates NK 212 sorghum by 37, 61 and 75% respectively. Similarly, heptachlor at 1·12 kg a.i./ha (10·42 g a.i./100 m of row) and lindane at 0·29 kg ...

A series of alkynyl maleimides were prepared via one-step cross-coupling reaction using bromomaleimide and acetylenes under the Sonogashira conditions, affording 1-((4-methoxyphenyl)-3-alkynes)-1H-pyrrole-2,5-diones in good to high yields. These products were subsequently converted in the corres...

A library of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides (7a–al) have been designed, synthesized and screened for their anti-proliferative activity against some selected human cancer cell lines namely DU-145, A-549, MCF-7 and HeLa. Most of them have shown promising...

This study aims to design and synthesize a novel harmine derivative N-(4-(hydroxycarbamoyl) benzyl)-1-(4-methoxyphenyl)-9H-pyrido [3,4-b]indole-3-carboxamide (HBC) as histone deacetylase (HDAC) inhibitor, and evaluate its antitumor activities and anti-metastasis mechanism. HBC not only exerted s...

Several novel trans-3-benzyl/(diphenyl)methyl/naphthylseleno substituted monocyclic β-lactams (5–7) have been synthesized in high yields. The reaction scheme inolves [2 + 2] cycloaddition (Staudinger) reaction between suitably substituted imines 4(a–h) and ketenes (B) accessed from 2-benzyl/(...

Stereoisomers of 1,2,3-triazole-functionalized, conformationally restricted β- or γ-amino esters with a cyclopentane skeleton were efficiently synthetized from the bicyclic β-lactam 6-azabicyclo[3.2.0]hept-3-en-7-one (1) and Vince γ-lactam (15) in five or six steps involving the azide–alkyn...

Chromanone-2-carboxylates and chroman-2-carboxylates are useful building blocks for the synthesis of a variety of bioactive compounds, such as repinotan, fidarestat, and nebivolol. An efficient and practical enantiospecific synthesis of chromanone-2-carboxylates and chroman-2-carboxylates has be...

Groups of rats were given metatartaric acid in the drinking-water in concentrations of 0 (control), 0·1, 0·5 or 3·0% for 18 wk. No effects associated with treatment were seen in the results of the haematological examinations and serum analyses. The treated animals consumed less water and food...

A new radioiodination reagent for the identification and quantitation of periodate-oxidized ribonucleosides was developed. The reagent, 3-([3-125I]iodo-4-hydroxyphenyl)propionyl carbohydrazide, was prepared by radioiodination of 3-(4-hydroxyphenyl)propionic acid N-hydroxysuccinimide ester in the...

Three (E/Z)-diastereoisomers, based on pyrrolo[2,3-b]quinoxaline system as fluorophore and containing: 2-thienylmethyl (1), bis(2-thienylmethyl)-2-aminoethyl (3a), bis(2-thienylmethyl)-3-aminopropyl (3b) groups as substituents, were synthesized and characterized by X-ray structural analysis, PXR...

In an approach to optimize 2-(4-fluorobenzylsulfanyl)-4-(2-thienyl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile (1a), a weak inhibitor of the cancer-related tyrosine kinase RET originating from a screening campaign, analogues with 3-thienyl substitution were prepared. Among the novel derivatives,...

The 3-(5-Bromo-2-thienyl)-1-(4-fluorophenyl)-3-acetyl-2-pyrazoline (2) (BTFA) was synthesized from condensation of thiophenechalcone (1) and hydrazine hydrate. The compound was characterized by FT-IR, 1H and 13C NMR. Crystal structure of this compound was determined using X-ray diffraction techn...

In this study, the novel sodium alginate/feather keratin-g-allyloxy polyethylene glycol (SA/FK-g-APEG) composite phase change fiber was designed and fabricated via centrifugal spinning for the first time. The chemical structure of the composite fiber was characterized by FT-IF and NMR, the therm...

BackgroundUrolithins are bioavailable products of gut microbiota metabolism of ellagitannins. Their biological activity includes anti-cancer effects.

A highly selective radical dioxygenation of alkenes using hydroxamic acid and O2 with 5–10 mol % of tert-butyl hydroperoxide as a catalyst was developed. On the basis of this newly developed strategy, a wide range of phenylethanol derivatives with a variety of functional groups can be effective...

Sodium borohydride is being considered as a chemical hydrogen storage material (hydrogen being released through hydrolysis) and as an anodic fuel for fuel cells. However, the current cost of sodium borohydride is prohibitively high for automotive applications. Thus, there is interest in recyclin...

H2 as an environmentally benign energy carrier could answer the world's continuously increasing demand for sustainable energy sources, especially in portable fuel cell applications. Thereby, H2 storage is the key issue. In the present work, we developed a liquid H2 storage material based on...

Sodium borohydride (NaBH4) is a complex hydride containing 10.5% of its mass as hydrogen; however, it is too stable to desorb hydrogen at room temperature. An ionic liquid (IL), vinylbenzyl trimethylammonium chloride, was applied to modify the charge distribution in BH4− and promote the dehydrog...

5-[2-(N,N-dimethylamino)ethoxy]-4,7-dimethylcoumarin (1) and 6-acetyl-5-[2-(N,N-dimethylamino)ethoxy]-4,7-dimethylcoumarin (2), structurally related, were synthesized using both conventional and microwave-assisted approach. An impact of acetyl groups on the molecular structure of coumarin deriva...