Furoxan sulfones and carbonitriles

A number of arylsulfonylfuroxan derivatives 43 (R = alkyl, aryl, alkoxy), have been studied, principally for their in vitro vasodilating and antiaggregatory properties [34, 35]. The involvement of NO in these actions has, in general, been evidenced through decreased activity in the presence of ODQ and/or Hb02. 

The derivatives bearing the arylsulfonyl groups at the 3- position of the ring proved to be more potent than the 4-arylsulfonyl substituted isomers, and the pair of isomeric phenyl-phenylsulfonylfuroxans (43a,b R=Q,I13) was more potent than the cor- 

A number ofwater soluble sulfonyl derivatives (44, X=S02, n=2,3) and some related compounds (44, X=Q,S, n=2,3) bearing a chain with a basic function at the ring, have 

The vasodilating potencies were, to a great extent, modulated within the series. A number of these products have been studied in vivo at the Cassella-Hoechst laboratories [38]. The best product was found to be derivative G95-6527 (44a, R QHs, X=S, n=2, R i =(df 3) when administered i.d. to anesthetised pigs it induced a significant decrease in both systolic and diastolic blood pressures (Fig. 6.2). The onset of the action was smooth and the maximum effect was reached after 30min and lasted for over 2h. 

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