Literature DB >> 17723300

Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.

Jonathan R Young1, Ronsar Eid, Cherilyn Turner, Robert J DeVita, Marc M Kurtz, Kwei-Lan C Tsao, Gary G Chicchi, Alan Wheeldon, Emma Carlson, Sander G Mills.   

Abstract

The preparation and structure-activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK(1) antagonists in vitro and efficacious in vivo with minimal interactions with P(450) liver enzymes. Oxadiazole analog 22 was determined to have excellent hNK(1) binding affinity, functional activity, and a good PD response in vivo.

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Year:  2007        PMID: 17723300     DOI: 10.1016/j.bmcl.2007.08.028

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


  3 in total

1.  Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.

Authors:  Steven Ballet; Debby Feytens; Koen Buysse; Nga N Chung; Carole Lemieux; Suneeta Tumati; Attila Keresztes; Joost Van Duppen; Josephine Lai; Eva Varga; Frank Porreca; Peter W Schiller; Jozef Vanden Broeck; Dirk Tourwé
Journal:  J Med Chem       Date:  2011-03-17       Impact factor: 7.446

2.  Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.

Authors:  Jolanta Dyniewicz; Piotr F J Lipiński; Piotr Kosson; Anna Leśniak; Marta Bochyńska-Czyż; Adriana Muchowska; Dirk Tourwé; Steven Ballet; Aleksandra Misicka; Andrzej W Lipkowski
Journal:  ACS Med Chem Lett       Date:  2016-11-01       Impact factor: 4.345

3.  Organocatalytic Enantioselective Conjugate Addition of Nitromethane to Benzylidene-2-Benzoyl Acetate: Asymmetric Synthesis of ABT - 627, an Endothelin Receptor Antagonist.

Authors:  Saumen Hajra; Sk Mohammad Aziz; Bibekananda Jana; Sunit Hazra
Journal:  Front Chem       Date:  2020-03-05       Impact factor: 5.221

  3 in total

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