Arylglyoxals condense with N-hydroxyurea in water via intermediate formation of N-hydroxy-N-[hydroxy(aroyl)]methylureas and 3,4,5-trihydroxy-5-arylimidazolidin-2-ones to yield 3-hydroxy-5-aryl-imidazolidine-2,4-diones as end products; the 3,4,5-trihydroxy-5-(p-chlorophenyl)imidazolidin-2-one and...

Imines of diethyl aminomalonate slowly dimerise imidazolidines in ethanol or methylene chloride at 40°C, but cycloaddition to other imines does not occur. Imines of glycine, alanine and phenylglycine methyl esters undergo rapid regio- and stereo-specific cycloaddition to methyl acrylate (MeCN, ...

A series of 5-tert-butyl-2-(pyridine-2-yl)imidazolidine-4-ones have been prepared and their Cu(II) complexes studied as enantioselective catalysts of the asymmetric Henry reaction of various aldehydes with nitromethane. It was found that these compounds were effective catalysts for this reaction...

Fourteen phthalazine-triones bearing different substituents at C-4 position were synthesized through multicomponent reactions (MCR) by using phthalhydrazide, dimedone and diferent aldehydes as starting materials, p-sulfonic acid calix[4]arene as catalyst and ethyl lactate as solvent under microw...

A new type of solid catalyst was prepared by coating a thin layer of policresulen, an inexpensive polymer prepared via condensation of 2-hydroxy-4-methylbenzenesulfonic acid and formaldehyde that has been used as commercially available drug, onto the surface of silica. The policresulen component...

Mesotrione (2-[4-(methylsulfonyl)-2-nithobenzoyl]-1, 3-cyclohexanedione) is a selective triketone herbicide that has been widely used in corn production for the past 15 years. However, its potential for risk to soil ecosystems is poorly documented. The present study investigated the soil enzyme ...

Mesotrione, an herbicide increasingly found in aquatic systems due to its increased application frequency in corn fields, is an inhibitor of the p-hydroxyphenylpyruvate dioxygenase (HPPD), a key enzyme for plastoquinone-9, α-tocopherol and indirectly for carotenoid biosynthesis. The direct effe...

The plant-derived biochars act as soil conditioners, and thus may influence biological interactions in the soil environment. However, their unintended negative and positive effects on soil organisms remain largely understudied. Therefore, we investigated the effect of 0, 1, 3, and 10% of wheat s...

Rats fed a low-protein diet and administered 2-(2-nitro-4-trifluoromethylbenzoyl)cyclohexane-1,3-dione (NTBC) orally at 30 μmol/kg/day (10 mg/kg/day) or fed a low-protein diet containing 5 ppm NTBC develop lesions to the cornea of the eye within 3–8 days of exposure with an incidence of about ...

Administration of a single oral dose of 2-(2-nitro-4-trifluoromethylbenzoyl)cyclohexane-1,3-dione (NTBC) to rats produced a marked tyrosinemia in the plasma and aqueous humor. The tyrosinemia was both time- and dose-dependent with the duration being more marked at the higher doses. The dose-resp...

The administration of the compound 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane- 1,3-dione (NTBC) to rats(10 mg/ kg body wt) caused an elevation in the concentration of plasma tyrosine and gave products in urine that were identified as 4-hydroxyphenylpyruvate (HPPA) and 4-hydroxyphenyllactat...

Administration of a single oral dose of 2-(2-nitro-4-trifluoromethyl-benzoyl)-cyclohexane-1,3-dione (NTBC) to mice increases the concentration of tyrosine in the plasma and aqueous humour. The tyrosinaemia is both time and dose-dependent with a single dose of 30 μmol NTBC/kg (10 mg/kg) producin...

2-(2-Nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione (NTBC) is a potent inhibitor of rat liver 4-hydroxyphenylpyruvate dioxygenase (HPPD) leading to tyrosinemia and corneal opacity. We examined the effect of NTBC on the extent of tyrosinemia and production of corneal lesions in the beagle ...

Until now, there are no publications about the preformulation studies on (S)-zaltoprofen ((S)-ZPF). Hence, we first investigated the solubility of (S)-ZPF, screened solubilizers and performed the pharmacokinetic study of (S)-ZPF in the presence of the solubilizers. The measurement of the solubil...

An efficient entry into pyrazol-3-ones is described starting from propenoic acids that were first transformed into the corresponding hydrazides. Oxidation of the hydrazides gave the diazenes and the latter cyclized to pyrazol-3-ones on treatment with ZrCl4. The methoxycarbonyl protection of the ...

Fourteen bergenin/cinnamic acid hybrids were synthesized, characterized and evaluated for their antitumour activity both in vitro and in vivo. The most potent compound, 5c, arrested HepG2 cells (IC50 = 4.23 ± 0.79 μM) in the G2/M phase and induced cellular apoptosis. Moreover, compound 5c was ...

The superelectrophilic activation of N-aryl amides of 3-arylpropynoic acids by Bronsted superacids (CF3SO3H, HSO3F) or strong Lewis acids AlX3 (X=Cl, Br) results in the formation of 4-aryl quinolin-2(1H)-ones in quantitative yields. The vinyl triflates or vinyl chlorides may be formed as additio...

The effect of the chlorine position on the C–Cl bond hydrogenolysis and the enantioselective hydrogenation of Cl substituted (E)-2,3-diphenylpropenoic acid derivatives has been studied over cinchonidine-modified Pd/Al2O3. In contrast to the fast hydrodechlorination of the β-phenyl-para-Cl subs...

The conjugated system of cinnamic acid, α-substituted with a phosphonoalkyl residue, was previously validated as a scaffold that provided one of the most potent organophosphorus inhibitors of bacterial urease. Following the idea of using Morita-Baylis-Hillman adducts to introduce the terminal p...

Nine organotin esters, Me2SnL2 1, Me3SnL 2, n-Bu2SnL2 3, n-Bu3SnL 4, Ph3SnL 5, (PhCH2)2SnL2 6, [(Me2SnL)2O]2 7, Et2SnL2 8 and n-Oct2SnL2 9, of (E)-3-(3-fluorophenyl)-2-(4-chlorophenyl)-2-propenoic acid, HL have been synthesized and characterized by elemental analysis, IR, Multinuclear NMR (1H, 1...