Literature DB >> 19640718

Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1.

Kristjan S Gudmundsson1, Paul R Sebahar, Leah D'Aurora Richardson, John F Miller, Elizabeth M Turner, John G Catalano, Andrew Spaltenstein, Wendell Lawrence, Michael Thomson, Stephen Jenkinson.   

Abstract

Several novel amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines were synthesized which had potent activity against HIV-1. The synthetic approaches adopted allowed for variation of the substitution pattern and resulting changes in antiviral activity are highlighted. This led to the identification of compounds with low and sub-nanomolar anti-HIV-1 activity.

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Year:  2009        PMID: 19640718     DOI: 10.1016/j.bmcl.2009.07.037

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


  9 in total

1.  Ligand-guided optimization of CXCR4 homology models for virtual screening using a multiple chemotype approach.

Authors:  Marco A C Neves; Sérgio Simões; M Luisa Sá e Melo
Journal:  J Comput Aided Mol Des       Date:  2010-10-20       Impact factor: 3.686

2.  Pharmacophore modeling, atom based 3D-QSAR and Molecular docking approaches to screen C-X-C chemokine receptor type 4 antagonists as microbicides for human immunodeficiency virus-1.

Authors:  Radhika Ramachandran; Shanmughavel Piramanyagam
Journal:  Virusdisease       Date:  2017-09-26

3.  Novel anti-inflammatory agents targeting CXCR4: Design, synthesis, biological evaluation and preliminary pharmacokinetic study.

Authors:  Renren Bai; Zhongxing Liang; Younghyoun Yoon; Eric Salgado; Amber Feng; Saumya Gurbani; Hyunsuk Shim
Journal:  Eur J Med Chem       Date:  2017-05-10       Impact factor: 6.514

Review 4.  Structural Analysis of Chemokine Receptor-Ligand Interactions.

Authors:  Marta Arimont; Shan-Liang Sun; Rob Leurs; Martine Smit; Iwan J P de Esch; Chris de Graaf
Journal:  J Med Chem       Date:  2017-03-10       Impact factor: 7.446

5.  Development of CXCR4 modulators by virtual HTS of a novel amide-sulfamide compound library.

Authors:  Renren Bai; Qi Shi; Zhongxing Liang; Younghyoun Yoon; Yiran Han; Amber Feng; Shuangping Liu; Yoonhyeun Oum; C Chris Yun; Hyunsuk Shim
Journal:  Eur J Med Chem       Date:  2016-11-24       Impact factor: 6.514

6.  Determination of the binding mode for the cyclopentapeptide CXCR4 antagonist FC131 using a dual approach of ligand modifications and receptor mutagenesis.

Authors:  S Thiele; J Mungalpara; A Steen; M M Rosenkilde; J Våbenø
Journal:  Br J Pharmacol       Date:  2014-12       Impact factor: 8.739

7.  5,6,7,8-Tetra-hydro-quinolin-8-one.

Authors:  Teodozja M Lipińska; Zbigniew Karczmarzyk; Waldemar Wysocki; Ewa Gruba; Andrzej Fruziński
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-05-07

8.  Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists.

Authors:  Mastaneh Safarnejad Shad; Sandra Claes; Eline Goffin; Tom Van Loy; Dominique Schols; Steven De Jonghe; Wim Dehaen
Journal:  Molecules       Date:  2021-10-18       Impact factor: 4.411

Review 9.  Small molecule inhibitors of CXCR4.

Authors:  Bikash Debnath; Shili Xu; Fedora Grande; Antonio Garofalo; Nouri Neamati
Journal:  Theranostics       Date:  2013-01-15       Impact factor: 11.556

  9 in total

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