Molecular modeling studies based on the potent NK-1 antagonist CP-96,345 led us to the identification of some 2-benzylidene- and 2-benzyl-3- benzylaminoquinuclidine derivatives as potential antagonists at the NK receptor subtypes. The synthesized compounds, whose Z/E isomerism has been defined by X-ray analysis, show only moderate potency on the three neurokinin receptors. The possible reasons of the low potency exhibited by the tested compounds are discussed.

Synthesis and neurokinin antagonist activity of 2-benzylidene- and 2- benzyl-3-benzylamino quinuclidines / Caliendo, Giuseppe; Greco, Giovanni; Perissutti, Elisa; Santagada, Vincenzo; Silipo, C.; Vittoria, A.; Turbanti, L.; Renzetti, A. R.; Benedetti, E.; Pedone, C.; Santini, A.. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 48:10(1993), pp. 1359-1378.

Synthesis and neurokinin antagonist activity of 2-benzylidene- and 2- benzyl-3-benzylamino quinuclidines

CALIENDO, GIUSEPPE;GRECO, GIOVANNI;PERISSUTTI, ELISA;SANTAGADA, VINCENZO;Santini A.
1993

Abstract

Molecular modeling studies based on the potent NK-1 antagonist CP-96,345 led us to the identification of some 2-benzylidene- and 2-benzyl-3- benzylaminoquinuclidine derivatives as potential antagonists at the NK receptor subtypes. The synthesized compounds, whose Z/E isomerism has been defined by X-ray analysis, show only moderate potency on the three neurokinin receptors. The possible reasons of the low potency exhibited by the tested compounds are discussed.
1993
Synthesis and neurokinin antagonist activity of 2-benzylidene- and 2- benzyl-3-benzylamino quinuclidines / Caliendo, Giuseppe; Greco, Giovanni; Perissutti, Elisa; Santagada, Vincenzo; Silipo, C.; Vittoria, A.; Turbanti, L.; Renzetti, A. R.; Benedetti, E.; Pedone, C.; Santini, A.. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 48:10(1993), pp. 1359-1378.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/565922
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