To understand better how [Leu]enkephalin (LE) acts to modulate learning and memory in rats, the plasma uptake, disappearance, and metabolism of LE were investigated following its intraperitoneal administration. Concentrations of [3H]-LE and its radioactive metabolites were determined by thin lay...

Using high-performance liquid chromatography with electrochemical detection to measure substrate disappearance and metabolite accumulation following addition of [Leu]enkephalin to samples prepared from chick brain in vitro, the following were found: 1.1. [Leu]enkephalin hydrolysis by whole foreb...

The effects of 1 mg of a synthetic analogue of leu-enkephalin (Dalargin) injected intramuscular twice daily for 3 consecutive days were studied in 20 patients with alcohol withdrawal syndrome. The results suggest that the therapeutic effects of Dalargin in alcohol withdrawal syndrome are mainly ...

4-(Methylnitrosamino)-l-(3-pyridyl)-1-butanone (NNK) and N-nitrosonornicotine (NNN), two tobacco specific nitrosamine carcinogens, can form adducts with DNA and proteins via pyridyloxobutylation upon phase I enzyme-mediated bioactivation. Such DNA modifications have been proposed as the root cau...

The reaction with β-trifluoromethyl acrylamide 3e and azomethine ylides generated from l-proline and several aldehydes provided the corresponding trifluoromethylated pyrrolizidines with excellent diastereoselectivity (>20/1) in all cases and moderate regioselectivity (up to 1/5.9). A DFT calcul...

The reductive coupling reaction between benzaldehyde and ethyl trifluoroacetate in the presence of magnesium and chlorotrimethylsilane in N-methyl-2-pyrrolidinone gave the acetal of the corresponding coupling compound in good yields. The yield of the coupling product largely depended on the benz...

The N,N-dimethylhydrazone of 1,1,1-trifluoroacetone, (E)-1,1-dimethyl-2-(1,1,1-trifluoropropan-2-ylidene)hydrazine, has been shown to undergo a diverse set of reactions following deprotonation with n-butyl-lithium; including alkylation, addition to ketones and aldehydes, as well as palladium-cat...

Reflecting the known biological activity of isoniazid-based hydrazones, seventeen hydrazones of 4-(trifluoromethyl)benzohydrazide as their bioisosters were synthesized from various benzaldehydes and aliphatic ketones. The compounds were screened for their in vitro activity against Mycobacterium ...

The first examples of thioether-substituted benzonitriles as potential soft-drug androgen receptor antagonists are reported. A number of 4-(alkylthio)- and of 4-(arylthio)-benzonitrile analogs were evaluated in human androgen receptor binding and cellular functional assays. Analogs with potent i...

A series of novel 1-[5-(4-methoxy-phenyl)-[1,3,4]oxadiazol-2-yl]-piperazine derivatives 8(a–o) were synthesized and characterized by elemental analyses, 1H NMR, 13C NMR and mass spectral studies. The newly synthesized compounds were screened for their anticonvulsant activity against maximal ele...

In the present study a series of new 1,3,4-oxadiazole derivatives containing 2-fluoro-4-methoxy moiety were synthesized. These newly synthesized compounds were characterized by NMR, mass spectral, IR spectral study and also by C, H, N analyses. All the newly synthesized compounds were screened f...

A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.02,6]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo.

A rapid and convenient method for the synthesis of 3,3-difluoroallylated diarylmethanes by reactions of diarylmethanes with α-(trifluoromethyl)styrenes in the presence of LiHMDS at room temperature was developed.

Publisher SummaryThis chapter covers bi- and tricyclic ring systems, highlighting recent development in the chemistry of bicyclic 6–6 systems containing one bridgehead nitrogen atom and one extra heteroatom and their benzologs. The members of these ring systems occupy valuable parts of the chem...

A short and efficient enantioselective synthesis of the HIV protease inhibitor amprenavir 1 (99% ee) as well as a formal synthesis of saquinavir 3 have been achieved in high enantiomeric purity starting from commercially available materials. Our strategy mainly comprises a Co-catalyzed two-stere...

Two diastereoisomers (2S,1′R) and (2R,1′R)-2-acetoxymethyl-3-phenyl-N-(1′-phenylethyl)-propionamide(2), have been studied to investigate their discrimination on the absolute configuration using nuclear magnetic resonance (NMR), infrared (IR) spectroscopy were performed. The experimental resul...

Despite the success which was achieved in the treatment of arterial hypertension, the problem remains actual. At the departments of pharmaceutical chemistry and pharmacology of the Zaporozhye State Medical Institute (Ukraine), our research team isolated the compound 1-(β-phenylethyl)-4-amino-1,...

Two chiral 2-azidoimidazolinium salts [(7aS)-3-azido-5,6,7,7a-tetrahydro-2-[(1R)-1-phenylethyl]-1H-pyrrolo[1,2-c]imidazolium hexafluorophosphate (2) and 2-azido-1,3-bis[(S)-1-phenylethyl]imidazolinium hexafluorophosphate (3)] were synthesized, and their structures were determined by X-ray single...

A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3–72 μM compared with the standard k...

In this paper the deamination mechanism of 1-(2-hydroxyl-1-phenylethyl)adenine (HPA) was studied using density functional method. As is known adenine has two possible forms under different pH values. One is the protonated amino form and the other is the neutral imino form. Through our calculatio...