Six new isoflavone-based esters, 7-decanoyloxy-3-(4′-substitutedphenyl)-4H-1-benzopyran-4-ones, derived from 1,3-benzenediol (resorcinol) and different para substituted phenylacetic acids have been synthesized and characterized. The molecular structures of the title compounds were elucidated wi...

Some 2-(diethylamino)-7-hydroxy-4H-1-benzopyran-4-one derivatives, potentially useful as activators of the cystic fibrosis transmembrane conductance regulator (CFTR), were prepared. The synthesized compounds were tested, together with others 2-(dialkylamino)-7-hydroxybenzopyran-4-one derivatives...

Eight new compounds, 7-alkyloxy-3-(4-alkyloxyphenyl)-4H-1-benzopyran-4-one incorporating isoflavone core and identical terminal side chains, OR (where R = CnH2n+1 with n ranging from 4 to 18 in even parity) have been synthesized and isolated. The thermal stability in relation to the phase behavi...

Series of flavones and methyl-4H-1-benzopyran-4-ones carrying mono or diamidinobenzimidazoles at different positions were synthesized and evaluated for antibacterial and antifungal activities against E. coli, S. aureus, MRSA (methicillin-resistant S. aureus), MRSE (methicillin-resistant S. epide...

In this paper, we report the inactivation of copper containing bovine plasma amine oxidase (BPAO) by a series of saturated alkylamines containing halogen atoms at γ-position, which are 1,1,1-trihalo-3-aminopropane, 1,1,1-trifluoro-2-hydroxy-3-aminopropane, 1,1,1-trichloro-2-hydroxy-3-aminopropa...

This paper examines the effects of in utero exposure to 2,4-dichlorophenyl-p-nitrophenyl ether (nitrofen) on the viability of neonatal Long-Evans rats. Oral administration of this herbicide on days 8–18 of gestation reduced neonatal survival and birth weight. Day 11 of gestation was the most se...

Studies on 2,4-dichlorophenyl-p-nitrophenyl ether (TOK®, a new selective herbicide, were undertaken in several animal species to characterize its toxicity. In rats, the single po LD50 ± SD value for technical grade TOK (95%) was 2.63 ± 0.13 g/kg as compared to 3.58 ± 0.14 g/kg for 100% TOK. I...

The administration of the herbicide 2,4-dichlorophenyl-p-nitrophenyl ether (nitrofen; NIT) to adult female mice by i.p. injection at doses of 500 and 1000 mgkgday for 3 days, reduced serum thyroxine (T4) levels. T4 levels were reduced in the high-dosage group by 60% of the control and by 20% in ...

A series of thiosemicarbazides with 4-nitrophenyl group was obtained in the reaction of carboxylic acid hydrazides with isothiocyanates. All compounds were checked for their antibacterial and antiproliferative activity. Our results have shown that derivatives 6-8 possessed antibacterial activity...

Novel palladium(II) and platinum(II) heterocycles were synthesized based 1,2-bis(3,5-dimethylisoxazol-4-ylmethylsulfanyl)ethane. According to X-ray Crystallographic data in molecule there are two bonds between divalent sulfur atoms and metal atom S-Pd-S to form a five-membered palladacycle in th...

The crystal structures of two Schiff base compounds, 2,6-dichlorobenzylidene-2,4-dichloroaniline (1) and 2,4-dichlorobenzylidene-2,4-dichloroaniline (2) have been determined from single-crystal X-ray diffraction and characterized by FT-IR and 1H NMR spectroscopy. The electronic structures of com...

Through exploration of the non-highly conserved allosteric hydrophobic pocket generated by DFG-out shifting in the inactive conformation, we discovered a highly selective type II PDGFRα kinase inhibitor 15i (CHMFL-PDGFRα-159), which exhibited strong potency against purified PDGFRα (IC50: 132 ...

An unexpected route for the synthesis of N,N-dialkyl formamidines has been reported by the reaction of amines with N,N-dialkyl formamides and phenyl chloroformate.

The amino acid-conjugates (1a–k) with eleven amino acids attached to primary amine of (S)-1-[1-(4-aminobenzoyl)-2,3-dihydro-1H-indol-6-sulfonyl]-4-phenyl-imidazolidin-2-one (DW2282, 1) were prepared and studied for their prodrug characteristics and anti-cancer activity against SW620 cell line. ...

Present work aimed to synthesize some unique bi-heterocyclic benzamides as lead compounds for the in vitro inhibition of urease enzyme, followed by in silico studies. These targeted benzamides were synthesized in good yields through a multi-step protocol and their structures were confirmed by IR...

FTIR spectra of dichloracetic acid and its eight complexes with substituted pyridine N-oxides and N,N-dimethylaniline in dichloromethane-d2 are reported. 4-N,N-dimethylaminopyridine N-oxides form two types of complexes with dichloroacetic acid; the acid interacts with NO or Me2N groups. The sh...

Acid–base equilibrium constants, i.e. acid dissociation, cationic homoconjugation and cationic heteroconjugation constants in 4-R-2,6-dimethylpyridine N-oxide systems (where R denotes methoxy-, methyl-, chloro- or nitro-group) in polar non-aqueous solvents: protophobic aprotic nitromethane, ace...

This paper describes the commercially-viable synthesis and isolation of 2-ethoxy-3-pyridylboronic acid on a ca. 70 g scale via a directed ortho-metalation reaction on readily-available 2-ethoxypyridine. A range of efficient cross-coupling reactions of 2-ethoxy-3-pyridylboronic acid with selected...

Fractionation of the carbohydrate-rich mucin present in the intestines of germ-free rats has been achieved on Dynospheres XP-3505. Comparison with Sepharose CL 4B shows that the separation on Dynospheres XP-3505 is better and quicker. The carbohydrate composition of the fractions show little dif...

Conditions which permit the dissociation of IgG-staphylococcal protein A interactions with resort to low pH buffers or the use of chaotropic ions are discussed in relation to: (a) the mechanism of the binding reaction; (b) the use of immobilised protein A for purification of cells or removal of ...