Literature DB >> 12713840

Structure-based approach to falcipain-2 inhibitors: synthesis and biological evaluation of 1,6,7-trisubstituted dihydroisoquinolines and isoquinolines.

Sanjay Batra1, Yogesh A Sabnis, Philip J Rosenthal, Mitchell A Avery.   

Abstract

1,4,7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1-benzyloxyphenyl-dihydroisoquinoline and -isoquinoline derivatives were found to exhibit better activity against falcipain-2 than their corresponding 1-hydroxyphenyl or 1-methoxyphenyl analogues. The docking scores correlate with the IC(50) values of compounds and give a high coefficient correlation of 0.94.

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Year:  2003        PMID： 12713840     DOI： 10.1016/s0968-0896(03)00117-2

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


  8 in total

1.  Falcipain-1, a Plasmodium falciparum cysteine protease with vaccine potential.

Authors:  Amit Kumar; Krishan Kumar; Reshma Korde; Sunil Kumar Puri; Pawan Malhotra; Virander Singh Chauhan
Journal:  Infect Immun       Date:  2007-01-22       Impact factor: 3.441

2.  Analysis of non-peptidic compounds as potential malarial inhibitors against Plasmodial cysteine proteases via integrated virtual screening workflow.

Authors:  Thommas M Musyoka; Aquillah M Kanzi; Kevin A Lobb; Özlem Tastan Bishop
Journal:  J Biomol Struct Dyn       Date:  2016-01-28

3.  Molecular docking and 3D-quantitative structure activity relationship analyses of peptidyl vinyl sulfones: Plasmodium Falciparum cysteine proteases inhibitors.

Authors:  Cátia Teixeira; José R B Gomes; Thierry Couesnon; Paula Gomes
Journal:  J Comput Aided Mol Des       Date:  2011-07-24       Impact factor: 3.686

4.  (+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.

Authors:  Sandeep Chaudhary; Stevan Pecic; Onica Legendre; Hérnan A Navarro; Wayne W Harding
Journal:  Bioorg Med Chem Lett       Date:  2009-03-16       Impact factor: 2.823

5.  Mining a cathepsin inhibitor library for new antiparasitic drug leads.

Authors:  Kenny K H Ang; Joseline Ratnam; Jiri Gut; Jennifer Legac; Elizabeth Hansell; Zachary B Mackey; Katarzyna M Skrzypczynska; Anjan Debnath; Juan C Engel; Philip J Rosenthal; James H McKerrow; Michelle R Arkin; Adam R Renslo
Journal:  PLoS Negl Trop Dis       Date:  2011-05-03

6.  Novel 5, 6-Dihydropyrrolo[2,1-a]isoquinolines as Scaffolds for Synthesis of Lamellarin Analogues.

Authors:  Shao Han Liao; Dai Hua Hu; Ai Ling Wang; De Peng Li
Journal:  Evid Based Complement Alternat Med       Date:  2011-08-07       Impact factor: 2.629

7.  2-(3,4-dihydro-4-oxothieno[2,3-d]pyrimidin-2-ylthio) acetamides as a new class of falcipain-2 inhibitors. 3. design, synthesis and biological evaluation.

Authors:  Jin Zhu; Tong Chen; Jie Liu; Ruoqun Ma; Weiqiang Lu; Jin Huang; Honglin Li; Jian Li; Hualiang Jiang
Journal:  Molecules       Date:  2009-02-16       Impact factor: 4.411

8.  2-amido-3-(1H-indol-3-yl)-N-substituted-propanamides as a new class of falcipain-2 inhibitors. 1. Design, synthesis, biological evaluation and binding model studies.

Authors:  Jin Zhu; Tong Chen; Lili Chen; Weiqiang Lu; Peng Che; Jin Huang; Honglin Li; Jian Li; Hualiang Jiang
Journal:  Molecules       Date:  2009-01-21       Impact factor: 4.411
  8 in total

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