Literature DB >> 19114307

Spiro-piperidine azetidinones as potent TRPV1 antagonists.

Dong Xiao1, Anandan Palani, Robert Aslanian, Brian A McKittrick, Andrew T McPhail, Craig C Correll, P Tara Phelps, John C Anthes, Diane Rindgen.   

Abstract

A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat.

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Year:  2008        PMID: 19114307     DOI: 10.1016/j.bmcl.2008.12.024

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


  2 in total

1.  Development of TsDPEN based imine-containing ligands for the copper-catalysed asymmetric Kinugasa reaction.

Authors:  Chuanlong Xu; Yuchen Yang; Yue Wu; Feilong He; Huakang He; Ping Deng; Hui Zhou
Journal:  RSC Adv       Date:  2020-05-12       Impact factor: 4.036

2.  Novel scaffolds for modulation of TRPV1 identified with pharmacophore modeling and virtual screening.

Authors:  Daria Goldmann; Peter Pakfeifer; Steffen Hering; Gerhard F Ecker
Journal:  Future Med Chem       Date:  2015       Impact factor: 4.767

  2 in total

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