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A series of  N -(arylpiperazinyl)acetamide derivatives of 1,3- and 3,7-dimethyl-1 H -purine-2,6(3 H ,7 H )-dione was synthesized and biologically evaluated in  in vitro  competition binding experiments for serotonin 5-HT 6 , 5-HT 7 , 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-HT 6 /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.

heterocyclic communications

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