Literature DB >> 19963378

Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.

Fabio M Sabbatini1, Romano Di Fabio, Cristiana Griffante, Giorgio Pentassuglia, Laura Zonzini, Sergio Melotto, Giuseppe Alvaro, Anna M Capelli, Lara Pippo, Elisabetta Perdona', Yves St Denis, Silvano Costa, Mauro Corsi.   

Abstract

A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK(1) antagonists. In particular, two of the compounds reported exhibited a good pharmacokinetic (PK) profile and produced anxiolytic-like effects in the gerbil foot tapping (GFT) in vivo model. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 19963378     DOI: 10.1016/j.bmcl.2009.11.078

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Fueling the Pipeline via Innovations in Organic Synthesis.

Authors:  Eric A Voight; Stephen N Greszler; Philip R Kym
Journal:  ACS Med Chem Lett       Date:  2021-08-27       Impact factor: 4.632

2.  Regiochemistry of cyclocondensation reactions in the synthesis of polyazaheterocycles.

Authors:  Patrick T Campos; Leticia V Rodrigues; Andrei L Belladona; Caroline R Bender; Juliana S Bitencurt; Fernanda A Rosa; Davi F Back; Helio G Bonacorso; Nilo Zanatta; Clarissa P Frizzo; Marcos A P Martins
Journal:  Beilstein J Org Chem       Date:  2017-02-10       Impact factor: 2.883

  2 in total

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