Literature DB >> 18068363

Development of CXCR3 antagonists. Part 4: discovery of 2-amino-(4-tropinyl)quinolines.

Roland L Knight1, Daniel R Allen, Helen L Birch, Gayle A Chapman, Frances C Galvin, Louise A Jopling, Christopher J Lock, Johannes W G Meissner, David A Owen, Gilles Raphy, Robert J Watson, Sophie C Williams.   

Abstract

The synthesis and biological evaluation of a novel series of 2-aminoquinoline substituted piperidines and tropanes incorporating a homotropene moiety is herein described. The series exhibits potent antagonism of the CXCR3 receptor and superior physicochemical properties. Compound 24d was found to be orally bioavailable, and PK/PD studies suggested it as a suitable tool for studying the role of CXCR3 in models of disease.

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Year:  2007        PMID: 18068363     DOI: 10.1016/j.bmcl.2007.11.075

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


  4 in total

1.  Palladium-Catalyzed Coupling of Functionalized Primary and Secondary Amines with Aryl and Heteroaryl Halides: Two Ligands Suffice in Most Cases.

Authors:  Debabrata Maiti; Brett P Fors; Jaclyn L Henderson; Yoshinori Nakamura; Stephen L Buchwald
Journal:  Chem Sci       Date:  2011-01-01       Impact factor: 9.825

Review 2.  Current trends and intricacies in the management of HIV-associated pulmonary tuberculosis.

Authors:  Narendran Gopalan; Padmapriyadarsini Chandrasekaran; Soumya Swaminathan; Srikanth Tripathy
Journal:  AIDS Res Ther       Date:  2016-09-26       Impact factor: 2.250

Review 3.  MAOS and medicinal chemistry: some important examples from the last years.

Authors:  Nailton M Nascimento-Júnior; Arthur E Kümmerle; Eliezer J Barreiro; Carlos A M Fraga
Journal:  Molecules       Date:  2011-11-07       Impact factor: 4.411

4.  Palladium-catalyzed amination of dichloroquinolines with adamantane-containing amines.

Authors:  Anton S Abel; Alexei D Averin; Olga A Maloshitskaya; Evgenii N Savelyev; Boris S Orlinson; Ivan A Novakov; Irina P Beletskaya
Journal:  Molecules       Date:  2013-02-06       Impact factor: 4.411

  4 in total

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