Abstract:
:An electrostatic interaction related to a favorable position of the distal phenyl ring and a phenylalanine residue in the binding pocket would explain the higher 5-HT1A affinity of a 4-phenyl-1,2,3,6-tetrahydropyridine (THP) analogue compared to the corresponding 4-phenylpiperazine analogue. To explore a possible reinforcement of this interaction to increase the affinity for 5-HT1A receptors, different 4-substituted-phenyl analogues were synthesized and tested. The most important increase of affinity is obtained with two electron-donating methyl groups in positions 3 and 5.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Liégeois JF,Lespagnard M,Meneses Salas E,Mangin F,Scuvée-Moreau J,Dilly Sdoi
10.1021/ml4004843subject
Has Abstractpub_date
2014-01-29 00:00:00pages
358-62issue
4issn
1948-5875journal_volume
5pub_type
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