N-(4-Arylpiperazinoalkyl)acetamide derivatives of 1,3- and 3,7-dimethyl-1H-purine-2,6(3H,7H)-diones and their 5-HT6, 5-HT7, and D-2 receptors affinity

作者：Zmudzki Pawel^*; Satala Grzegorz; Chlon Rzepa Grazyna; Bojarski Andrzej J; Popik Piotr; Zajdel Pawel

来源：Heterocyclic Communications, 2015, 21(1): 13-18.

DOI：10.1515/hc-2014-0200

• 5-HT6 receptor ligands
• 5-HT7 receptor ligands
• D-2 receptor ligands
• long-chain arylpiperazines
• theobromine
• theophylline

A series of N-(arylpiperazinyl) acetamide derivatives of 1,3- and 3,7-dimethyl-1H-purine-2,6(3H,7H)-dione was synthesized and biologically evaluated in in vitro competition binding experiments for serotonin 5-HT6, 5-HT7, and dopamine D-2 receptors. The structure-affinity relationships for this group of compounds allowed for determination of structural features responsible for receptor affinity. Among the investigated derivatives, compounds 5 and 12 with (2,3-dichlorophenyl) piperazine moiety were classified as potent dual 5-HT6/D-2 receptors ligands, whereas compound 4, with 4-(benzo[d]isothiazol-3-yl) piperazine moiety, and compounds 8 and 15, with (2,3-dichlorophenyl) piperazine moiety, were classified as potent D-2 receptor ligands.

• 出版日期2015-2