Literature DB >> 18417342

A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.

Laura De Luca1, Maria Letizia Barreca, Stefania Ferro, Nunzio Iraci, Martine Michiels, Frauke Christ, Zeger Debyser, Myriam Witvrouw, Alba Chimirri.   

Abstract

We report herein the development of a new three-dimensional pharmacophore model for HIV-1 integrase inhibitors which led to the discovery of some 4-[1-(4-fluorobenzyl)-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acids that are able to specifically inhibit the strand transfer step of integration at nanomolar concentration. The synthesis of the new designed molecules is also described.

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Year:  2008        PMID： 18417342     DOI： 10.1016/j.bmcl.2008.03.089

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


  6 in total

1.  Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited.

Authors:  Jing Tang; Kasthuraiah Maddali; Yves Pommier; Yuk Y Sham; Zhengqiang Wang
Journal:  Bioorg Med Chem Lett       Date:  2010-04-21       Impact factor: 2.823

2.  Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors.

Authors:  Stefania Ferro; Sara De Grazia; Laura De Luca; Rosaria Gitto; Caterina Elisa Faliti; Zeger Debyzer; Alba Chimirri
Journal:  Molecules       Date:  2011-08-11       Impact factor: 4.411

Review 3.  Computer tools in the discovery of HIV-1 integrase inhibitors.

Authors:  Chenzhong Liao; Marc C Nicklaus
Journal:  Future Med Chem       Date:  2010-07       Impact factor: 3.808

4.  6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase.

Authors:  Jing Tang; Kasthuraiah Maddali; Christine D Dreis; Yuk Y Sham; Robert Vince; Yves Pommier; Zhengqiang Wang
Journal:  Bioorg Med Chem Lett       Date:  2011-02-18       Impact factor: 2.823

5.  Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.

Authors:  Anneleen Hombrouck; Barbara Van Remoortel; Martine Michiels; Wim Noppe; Frauke Christ; Anders Eneroth; Britt Louise Sahlberg; Kurt Benkestock; Lotta Vrang; Nils Gunnar Johansson; Maria Letizia Barreca; Laura De Luca; Stefania Ferro; Alba Chimirri; Zeger Debyser; Myriam Witvrouw
Journal:  Antimicrob Agents Chemother       Date:  2008-06-09       Impact factor: 5.191

Review 6.  A review on recent developments of indole-containing antiviral agents.

Authors:  Ming-Zhi Zhang; Qiong Chen; Guang-Fu Yang
Journal:  Eur J Med Chem       Date:  2014-10-23       Impact factor: 6.514
  6 in total

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