Fujio Saito

Synthesis and collateral dilator activity of nitroxyalkylamides having direct or latent sulfhydryl moieties.

To develop an orally active, long-acting nitrate that does not induce tolerance, nitroxyalkyl compounds were prepared and their activities evaluated by the use of carotid collaterals in anesthetized dogs. A compound having a favorable pharmacological profile, that is, long-lasting collateral vasodilatation and little hypotension, and lack of nitrate tolerance, was chosen for further evaluation.

Synthesis of fused aminotetrahydrocarbazole compounds

Intramolecular Diels-Alder reaction of 3-(1H-indol-3-yl)-2-propenoates having olefinic substituents as the 1-position of the indole ring gave stereoselectively pentacyclic fused indole compounds in good yield. Aminotetrahydrocarbazoles derivatives (8,21,22) were obtained by Curtius rearrangment via carboxylic acid derivatives. Some of these compounds showed intersting pharmacological activity such as antiarrhytmic activity.

An efficient synthesis of γ-lactones as precursors of hydroxyethylene dipeptide isostere

An efficient and stereocontrolled synthesis of γ-lactones as precursors of the hydroxyethylene dipeptide isostere has been developed, starting from readily available 5-oxotetrahydrofuran-2-carboxylic acid 6.