Synthesis of some thiazolyl-pyrazoline derivatives and preliminary investigation of their hypotensive activity.

Some 1-(4-arylthiazol-2-yl)-3,5-diaryl-2-pyrazoline derivatives were synthesized by reacting 1-thiocarbamoyl-3,5-diaryl-2-pyrazoline derivatives with phenacetylbromide in ethanol. The structural elucidation of the compounds were performed by IR, 1H-NMR and Mass spectral data and elemental analyses. The hypotensive activities of 13 compounds were evaluated by using the tail-cuff method. All examined compounds showed appreciable hypotensive activities. Clonidine was used as reference substance in the pharmacological evaluation.

Some of the amino acid chemistry going on in the Laboratory of Amino Acids, Peptides and Proteins.

Some of the chemistry of amino acids going on in our laboratory (Laboratoire des Amino acides Peptides et Protéines) is described as well as some mass spectrometry methodology for their characterization particularly on solid supports. Several aspects are presented including: (i) the stereoselective synthesis of natural and unnatural amino acids using 2-hydroxypinan-3-one as chiral auxiliary; (ii) the stereoselective synthesis of natural and unnatural amino acids by deracemization of alpha-amino acids via their ketene derivatives; (iii) the synthesis of alpha-aryl-alpha-amino acids via reaction of organometallics with a glycine cation; (iv) the diastereoselective synthesis of glycosyl-alpha-amino acids; (v) the synthesis of beta-amino acids using alpha-aminopyrrolidinopiperazinediones as chiral templates; (vi) the reactivity of urethane-N-protected N-carboxyanhydrides. To characterize natural and non natural amino acids through their immonium ions by mass spectrometry, some methodology is also described.

Synthesis of some chroman derivatives and preliminary investigation on their vasodilatory activity.

In this study, some N'-(chroman-4-yliden)-4-aryl-2-thiazolylhidrazide derivatives were synthesized. Their structures were elucidated by IR, NMR and microanalyses. The vasodilatory activities of the compounds obtained were examined in vitro.

Synthesis of some 1-(2-arylvinyl)-3-arylpyrazino[1,2-a]benzimidazole derivatives and their antimicrobial activities.

Some 1-(2-arylvinyl)-3-arylhyrazino[1,2-a]benzimidazole derivatives were synthesized, their structures were elucidated, and their antibacterial and antifungal activities were examined. None of the compounds proved to be sufficiently active.

Synthesis and antiarrhythmic properties of basic amide derivatives of imidazolidine-2,4-dione and pyrrolidine-2,5-dione II.

Basic amide derivatives of imidazolidine-2,4-dione and pyrrolidine-2,5-dione were synthesized as potential antiarrhythmic agents. Some of them have shown antiarrhythmic activity in the chloroform, barium chloride or adrenaline induced arrhythmia.

Infrared, raman, and 13C NMR spectra of two crystalline forms of (1R,3S)-3-(p-thioanisoyl)-1,2,2-trimethylcyclopentanecarboxylic acid.

A comparative structural analysis of the two polymorphic forms of (1R,3S)-3-(p-thioanisoyl)-1,2,2-trimethylcyclopentanecarboxylic acid has been performed with infrared, Raman, and 13C NMR spectroscopy. The results are compared with those of the crystallographic and thermal studies on the two forms published in previous papers. The enantiotropism of the polymorphs as well as the differences in the conformation of the carboxyl group and the resulting intermolecular hydrogen bonds were confirmed by the infrared and Raman studies.

Comparative study of the two polymorphic forms of p-(1R,3S) 3-thioanisoyl-1,2,2-trimethylcyclopentane carboxylic acid.

The crystal structure of polymorph I of p-(1R,3S)3-thioanisoyl-1,2,2-trimethylcyclopentane carboxylic acid has been determined and is compared with that of polymorph II that was previously described. Polymorph I is very different at the level of the carboxyl group. It does not present disorder and the values found for the C-O bonds correspond exactly to single and double bond lengths. In addition, the carboxyl groups of the two molecules in the cell packing are involved in symmetric hydrogen bonds [2.662(6) A] leading to the formation of a dimer around the twofold axis following x with a shift on z. The different conformations on the carboxylic group between the two polymorphs are in good agreement with the thermodynamic study.

Synthesis and vasodilatory activity of some thiazolo-triazole derivative.

In this study, some thiazolo[3,2-b]-1,2,4-triazole derivatives were synthesized. Their vasodilatory activities were examined in vitro. All examined compounds showed appreciable activity.

Synthesis and pharmacological properties of phenoxyethylpiperazine derivatives.

Salts of new 1-phenoxyethylpiperazines 1-5, their 4-amidine derivatives 6-10 and 4-phenoxyacetyl derivatives 11-15 have been obtained. Some of them were screened for their cardiovascular activity.