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Literature DB >> 16723225

Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.

Haolun Jin¹, Ruby Z Cai, Laura Schacherer, Salman Jabri, Manuel Tsiang, Maria Fardis, Xiaowu Chen, James M Chen, Choung U Kim.

Abstract

A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational analysis of 1,6-naphthyridine carboxamide compound L-870810 and docking the designed inhibitor into the active site of our integrase enzyme model. The efficient syntheses of pyrroloquinoline tri-cyclic analogs are described. The SAR studies resulted in the identification of a lead compound that is more potent and more soluble than L-870810.

Entities: Chemical Gene

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Year: 2006 PMID： 16723225 DOI： 10.1016/j.bmcl.2006.05.016

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

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Cited

8 in total

1. Computational design of a full-length model of HIV-1 integrase: modeling of new inhibitors and comparison of their calculated binding energies with those previously studied.

Authors: Selami Ercan; Necmettin Pirinccioglu
Journal: J Mol Model Date: 2013-08-02 Impact factor: 1.810

2. Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction.

Authors: Erik Serrao; Bikash Debnath; Hiroyuki Otake; Yuting Kuang; Frauke Christ; Zeger Debyser; Nouri Neamati
Journal: J Med Chem Date: 2013-03-18 Impact factor: 7.446

Review 3. Therapeutic strategies underpinning the development of novel techniques for the treatment of HIV infection.

Authors: Jian J Tan; Xiao J Cong; Li M Hu; Cun X Wang; Lee Jia; Xing-Jie Liang
Journal: Drug Discov Today Date: 2010-01-22 Impact factor: 7.851

4. Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.

Authors: Gregg S Jones; Fang Yu; Ameneh Zeynalzadegan; Joseph Hesselgesser; Xiaowu Chen; James Chen; Haolun Jin; Choung U Kim; Matthew Wright; Romas Geleziunas; Manuel Tsiang
Journal: Antimicrob Agents Chemother Date: 2008-12-22 Impact factor: 5.191

5. Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones.

Authors: Xue Zhi Zhao; Kasthuraiah Maddali; B Christie Vu; Christophe Marchand; Stephen H Hughes; Yves Pommier; Terrence R Burke
Journal: Bioorg Med Chem Lett Date: 2009-03-28 Impact factor: 2.823

Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.

1. Computational design of a full-length model of HIV-1 integrase: modeling of new inhibitors and comparison of their calculated binding energies with those previously studied.

2. Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction.

Review 3. Therapeutic strategies underpinning the development of novel techniques for the treatment of HIV infection.

4. Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.

5. Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones.

6. Diketoacid-genre HIV-1 integrase inhibitors containing enantiomeric arylamide functionality.

Review 7. Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity.

Review 8. Raltegravir, elvitegravir, and metoogravir: the birth of "me-too" HIV-1 integrase inhibitors.