Literature DB >> 24837158

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists.

Shinya Nagashima1, Yuji Matsushima2, Hisao Hamaguchi2, Hiroshi Nagata2, Toru Kontani2, Ayako Moritomo2, Tadatsura Koshika2, Makoto Takeuchi2.   

Abstract

Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action in a rat model than tiotropium bromide.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  ASP9133; COPD; In vivo selectivity; Long acting muscarinic receptor antagonist

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Year:  2014        PMID: 24837158     DOI: 10.1016/j.bmc.2014.04.031

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  1 in total

Review 1.  Recent Advances in the Synthesis of Oxazole-Based Molecules via van Leusen Oxazole Synthesis.

Authors:  Xunan Zheng; Wei Liu; Dawei Zhang
Journal:  Molecules       Date:  2020-03-31       Impact factor: 4.411

  1 in total

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