| Literature DB >> 23466604 |
Andrea Cappelli1, Monica Manini, Salvatore Valenti, Federica Castriconi, Germano Giuliani, Maurizio Anzini, Simone Brogi, Stefania Butini, Sandra Gemma, Giuseppe Campiani, Gianluca Giorgi, Laura Mennuni, Marco Lanza, Antonio Giordani, Gianfranco Caselli, Ornella Letari, Francesco Makovec.
Abstract
A new class of serotonin 5-HT1A receptor ligands related to NAN-190, buspirone and aripiprazole has been designed using our potent 5-HT3 receptor ligands as templates. The designed pyrrolidone derivatives 10a-n were prepared by means of the straightforward chemistry consisting in the reaction of the appropriate γ-haloester derivatives with the suitable arylpiperazinylalkylamines. The nanomolar 5-HT1A receptor affinity and the agonist-like profile shown by fused pyrrolidone derivatives 10k,m stimulated the rationalization of the interaction with an homology model of the 5-HT1A receptor and the evaluation of their selectivity profiles and the pharmacokinetic properties. Interestingly, the results of the profiling assays suggested for close congeners 10k,m a significantly divergent binding pattern with compound 10m showing an appreciable selectivity for 5-HT1AR.Entities:
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Year: 2013 PMID： 23466604 DOI： 10.1016/j.ejmech.2013.01.044
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514