Synthesis and structure-activity relationships of a new model of arylpiperazines. Part 7: Study of the influence of lipophilic factors at the terminal amide fragment on 5-HT(1A) affinity/selectivity |
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Authors: | López-Rodríguez María L Ayala David Viso Alma Benhamú Bellinda de La Pradilla Roberto Fernández Zarza Fernando Ramos José A |
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Institution: | Departamento de Química Orgánica I, Facultad de Ciencias Químicas, Universidad Complutense, E-28040 Madrid, Spain. mluzlr@quim.ucm.es |
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Abstract: | The influence of lipophilic factors at the amide fragment of a new series of (+/-)-7a-alkyl-2-4-(4-arylpiperazin-1-yl)butyl]-1,3-dioxoperhydropyrrolo1,2-c]imidazoles 2 and of (+/-)-7a-alkyl-2-(4-arylpiperazin-1-yl)methyl]-1,3-dioxoperhydropyrrolo1,2-c]imidazoles 3 has been studied. Variations of logP have been carried out by introducing different hydrocarbonated substituents (R(1)) at the position 7a of the bicyclohydantoin, namely the non-pharmacophoric part. All the new compounds exhibit high potency for the 5-HT(1A) receptor; however, affinities for the alpha(1) receptor are high for compounds 2a-l while compounds 3a-f are selective over this adrenergic receptor. On the other hand, differences in logP do not notably affect the K(i) values for the above receptors. |
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