SYNTHESE D'UN ANALOGUE DU FOSTEDIL: LE DIETHYL 4-(1,2,3-DIAZAPHOSPHOL- 5-YL)BENZYLPHOSPHONATE. ETUDE DE SON ACTIVITE INHIBITRICE DU TRANSPORT CALCIQUE A TRAVERS LES MEMBRANES BIOLOGIQUES

Abstract

Nous decrivons la synthese en quatre stapes d'analogues d'un inhibiteur calcique, le Fostedil, a atome de phosphore dicoordonne: les diethyl-4 (1,2,3-diazaphosphol-5-yl)benzylphosphonates 6, oil nous avons remplace le motif benzothiazole du Fostédil I, par un cycle 1,2,3-diazaphosphole. L'activitE inhibitrice du transfert de calcium it travers les membranes biologiques, des composes 6, s'avere faible.

Mots cles: 1,2,3-Diazaphospholes; analogues du Fostédil, Inhibiteur calcique.

We describe a four step synthesis of dicoordinated phosphorus Fostedil analogues: the diethyl-4 (1,2,3-diazaphosphol-5-yl)benzylphosphonates 6, in which the benzothiazole Fostedil group is replaced by a 1,2,3 diazaphosphole ring. Inhibitive activity of calcium transfert, through biological membranes, of compounds 6 is weak.

Key Words:

• 1,2,3-Diazaphospholes
• Fostedil analogues
• calcium antagonist.