Antoine Ezhaya

Solid-phase synthesis of 3-hydroxymethyl isoxazoles via resin bound nitrile oxides

Abstract [3+2] Cycloaddition of alkynes to resin bound nitrile oxides gives after cleavage of 3,4,5 trisubstituted isoxazoles in acceptable yields and fair to good purity, depending on the alkyne substituents. The reaction has been automated on the ACT 496 synthesiser.

Anti-secretory and anti-ulcer activities of some new 2-(2-pyridylmethyl-sulfinyl)-benzimidazoles

Abstract A series of substituted sulfinyl benzimidazoles were prepared and tested for gastric anti-secretory activity. Following initial screening, two compounds were tested for anti-ulcer activity. The new compounds showed pharmacological properties different from those of omeprazole 1 , since they proved to be weak anti-secretory agents displaying non-specific anti-ulcer activity. Some structural requirements for optimum activity were elucidated.

New pyrrolidin-, piperidin- and azepin-2-oxocarboxylic acid esters are preferential M1, M3 muscarinic antagonists. Synthesis and bronchospasmolytic activity

A series of new 3-tropanol and 3-quinuclidinol esters of phenyl-substituted pyrrolidin-, piperidin- and azepin-2-oxocarboxylic acid were synthesized and tested for antimuscarinic activity. The compounds showed a preferential in vitro activity at M1 and M3 receptor subtypes and an interesting activity profile in vivo. A potential use as selective bronchospasmolytic agents has been suggested for selected compounds.