A series of novel 2-(5-aminomethylene-4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropionic acid ethyl esters has been synthesized. Target compounds were evaluated for their trypanocidal activity towards Trypanosoma brucei brucei and Trypanosoma brucei gambiense. Several hit-compounds (8, 10, 12) in...

The gas chromatographic retention behaviour of C3C5 saturated branched-chain, C3C6 unsaturated, ethyl and 2-chloro-, 2,2-dichloro- and 2,2,2-trichloroethyl esters of benzoic, 4-nitrobenzoic and 3,5-dinitrobenzoic acids on SE-30 and OV-351 capillary columns at several temperatures is reported...

CuI-2-(2′-pyridyl)benzimidazole catalyst system can serve efficiently to promote N-arylation of various indoles to afford the N-arylated indoles. The bidentate ligand, 2-(2′-pyridyl)benzimidazole was proved superior to monodentate nitrogen-based ligands and well-known bidentate ligands such as...

Exposure of ethyl 2-cyano-3-(2-methoxy-5-nitrophenyl)acrylate 1f to triethylamine in hot ethanol resulted in the formation of the dihydro derivative 2f and vinylogue 3f in high yields. Single crystal X-ray data are provided for 3f. Similar reactions were observed for various analogues. The react...

A method for the combinative oxidative homo dimerization and cyanation of free indole derivatives catalysed by TEMPO along with silver carbonate was demonstrated for the first time This new methodology is both atom and step efficient and is applicable to a broad scope of substrates, allowing the...

A highly discrete distribution of neurohypophyseal hormone receptors was discovered in the mammalian and avian brain. These receptors are heterogeneous. In rat brain oxytocin (OT) and V1a receptors can be distinguished which bind OT with an order of magnitude difference in affinity and which are...

The distribution and characteristics of putative arginine vasotocin (AVT) receptors in the urodele amphibian kidney were investigated using in vitro quantitative autoradiography. Specific binding sites for [3H]arginine vasopressin (AVP) in the kidneyof the rough-skinned newt (Taricha granulosa) ...

Although neurohypophysial peptides are present in many regions of the developing and adult bullfrog (Rana catesbeiana) brain, the function of these peptides remains unclear. To investigate possible behavioral actions, we examined locomotor activity following peptide injection in bullfrogs at var...

Approximately 70 anthraquinones and 20 benzanthrones were assayed for mutagenicity in the Salmonella/microsome test, employing 5 tester strains and Aroclor 1254 induced rat-liver microsomes. About one-third of the anthraquinones were frameshift mutagens, particularly phenolic and nitro anthraqui...

The absolute configuration of two novel αvβ6 integrin inhibitors was established via degradation to the corresponding C3-aryl substituted butyrolactone. The configuration of the resulting lactones was established by asymmetric synthesis using 1,4-addition of arylboronic acids to butenolide, ca...

In this article, we report novel leukotriene (LT) biosynthesis inhibitors that may target 5-lipoxygenase-activating protein (FLAP) based on the previously identified isoxazole derivative (8). The design and synthesis was directed towards a subset of 4,5-diaryl-isoxazole-3-carboxylic acid derivat...

1.1. Urine samples from healthy humans have been analysed for branched shortchain dicarboxylic acids using combined gas-liquid chromatography-mass spectrometry.2.2. Methylsuccinic, 3-methylglutaric, 3-methylhexanedioic, 3-methylheptanedioic, and 3-methyloctanedioic acid were present in all urine...

The mass spectra of the dimethyl esters of some aliphatic 3-methyl-α,ω-dicarboxylic acids show no molecular ion. The highest mass peak is due to α-cleavage with loss of a methoxy radical. Except for the lower homologue, loss of methanol is of low importance, but the metastable peak for the pr...

Diaryl piperazine acetamides were identified as potent and selective dopamine D4 receptor agonists. Our strategy is based on an amide bond reversal of an acid sensitive, dopamine D4 receptor partial agonist, PD 168077. This reversal provided compounds with excellent potency and improved stabilit...

The optimized molecular structure, vibrational frequencies, corresponding vibrational assignments of the title compound have been investigated experimentally and theoretically. The HOMO and LUMO analysis is used to determine the charge transfer within the molecule. The stability of the molecule ...

The synthesis of enantiomerically pure (+)- and (-)-2-methoxy-4-(S-methyl-N-[(4-methylphenyl)-sulfonyl]-sulfonimidoyl)-benzoic acid 4a was carried out. The chemical correlation of (+)-(S)-S-methyl-N-[(4-methylphenyl)-sulfonyl]-4-methyl-phenyl)-sulfoximide 13 with (+)-4a was undertaken. The absol...

The ethanolic extract of the root of Berberis umbellata yielded 2,5-bis-(2′-methoxy-5′-methylphenyl)-furan which has not been previously isolated from a natural source.

The triphenyltin and tri-n-butyltin complexes of some 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids have been synthesized and characterized by 1H-, 13C-, 119Sn-NMR, IR and 119mSn Mössbauer spectroscopic techniques in combination with elemental analysis. The crystal structures of triphenylti...

Reaction of the laterally lithiated (S)-4-isopropyl-2-(2-methoxy-6-methylphenyl)oxazoline with p-tolualdehyde gave an inseparable mixture of the addition products in low diastereoselectivity. However, the (S,S)-product cyclized to the corresponding 3,4-dihydroisocoumarin faster than the (S,R)-pr...

A light-yellow crystalline product (1), which was isolated after one week from the filtrate of the reaction between S-2-methylbenzyldithiocarbazate and 2,3-dihydroxybenzaldehyde, was characterised by single crystal X-ray diffraction, FTIR and NMR spectroscopic analyses. The experimental molecula...