Naphthosultam Derivatives: A New Class of Potent and Selective 5-HT2 Antagonists.-A series of 2-aminoalkyl-1,8-naphthosultams such as (V) is prepared by consecutive coupling of 1,8-naphthosultam (I) with the dihalides (II) and the corresponding secondary amines (IV). Among these, the derivative (Ve) shows the highest 5-HT2 receptor affinity. -(MALLERON, J.-L.; COMTE, M.-T.; GUEREMY, C.; PEYRONEL, J. F.; TRUCHON, A.; BLANCHARD, J. C.; DOBLE, A.; PIOT, O.; ZUNDEL, J.-L.; HUON, C.; MARTIN, B.; MOUTON, P.; VIROULAUD, A.; ALLAM, D.; BETSCHART, J.; J. Med. Chem. 34 (1991) 8, 2477-2483; Dep. Chim. Pharm. Biol., Centre Rech. Vitry Alfortville Rhone-PoulencRorer, 94403 Vitry-sur-Seine, Fr.; EN)
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