Substituted 3-amino and/or 3-aminomethyl-3, 4-dihydro-2H-1-benzopyrans: synthesis and biological activity

…, B Pfeiffer, MC Rettori, P Renard, G Guillaumet

Index: Comoy, Corinne; Guerin, Virginie; Pfeiffer, Bruno; Rettori, Marie-Claire; Renard, Pierre; Guillaumet, Gerald Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 3 p. 483 - 495

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Citation Number: 12

Abstract

A series of new 3-amino, 3-aminomethyl-5-alkoxy-3, 4-dihydro-2H-1-benzopyran and 5′- alkoxy-3′, 4′-dihydrospiro [piperazine-2, 3′(2′ H)-benzopyran] derivatives was prepared and evaluated for affinity at 5-HT1A, 5-HT2A and D2 receptors. Two of the compounds (1f and 2b) can be considered as potent and selective 5-HT2A ligands. One compound (1g) demonstrated high affinity for 5-HT1A and D2 receptor binding sites and ...