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J M Morand

Publications and source records attributed to J M Morand.

14 recordsLinked to original sources
PubMed2000

Synthesis and alpha-adrenergic binding ligand affinities of 2-iminoimidazolidine derivatives.

In order to obtain possible veinotonic drugs acting through alpha2 receptor activation, we prepared clonidine analogues in which the 2-imino-imidazolidine was attached to various aliphatic or aromatic heterocycles. Among them, the two benzopyranic derivatives 16 and 22 exhibited interesting affinities (19 and 95 nM respectively on [3H]rauwolscine binding, compared to 35 nM for clonidine). Their affinity for alpha1 receptors was found to be much lower: 7570 and 5030 nM for 16 and 22 respectively, suggesting 16 to be 400 times more selective for alpha2 than for alpha1-adrenoceptors.

Adrenergic alpha-2 Receptor Agonists↗
PubMed1998

Synthesis, activity, and molecular modeling of new 2, 4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors.

A series of 2,4-dioxo-5-(2-naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues have been prepared as aldose reductase inhibitors. In vitro inhibitory activities of bovine lens aldose reductase were determined by a conventional method. 1-Naphthyl-substituted derivatives of the 2-thioxo series were the more potent inhibitors (IC50 congruent with 10 nM) with similar activity to that of Epalrestat. Structural analysis, especially by X-ray crystallography of two selected compounds, and molecular modeling comparisons with Zopolrestat were performed. These results provide explanations of the good activity of the inhibitor, the preference for 1-naphthyl-substituted compounds, and the nature of molecular interactions in these systems.

Acetates↗
PubMed1992

[Biotransformation of aza-3-chalcol in the rat: isolation and structural analysis of seven metabolites].

The azachalcol 3-phenyl-1-(3-pyridinyl)prop-2-en-1-ol S-1 has been used to investigate the metabolic profile in rat. Seven metabolites and the unchanged substance were isolated from urine. The biotransformation products were extracted and purified by chromatography (LC, CTLC, HPLC) and identified by comparison with some synthetic reference compounds or by spectroscopic analysis (UV, IR, 1H, 13C NMR and MS). A scheme of potential metabolic pathway is proposed. It appears that three specific targets of the parent molecule are extensively oxidized. Thus the aromatic heterocycle yields three N-oxides (M-4, M-5, M-7). The deshydrogenation of the secondary alcoholic group to the ketone is also observed (M-2). Finally, the ethylenic double bond is a favored site for hydroxylation (M-7, M-8) as well as reduction (M-3, M-4, M-6).

Animals↗