Literature DB >> 11451529

Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase.

F Zuccotto1, M Zvelebil, R Brun, S F Chowdhury, R Di Lucrezia, I Leal, L Maes, L M Ruiz-Perez, D Gonzalez Pacanowska, I H Gilbert.   

Abstract

There is an urgent need for the development of new drugs to treat Chagas' disease, which is caused by the protozoan parasite Trypanosoma cruzi. The enzyme dihydrofolate reductase (DHFR) has been a very successful drug target in a number of diseases and we decided to investigate it as a potential drug target for Chagas' disease. A homology model of the enzyme was used to search the Cambridge Structural Database using the program DOCK 3.5. Compounds were then tested against the enzyme and the whole parasite. Compounds were also screened against the related parasite, Trypanosoma brucei.

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Year:  2001        PMID： 11451529     DOI： 10.1016/s0223-5234(01)01235-1

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  6 in total

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2.  Receptor-Based Discovery of a Plasmalemmal Monoamine Transporter Inhibitor via High Throughput Docking and Pharmacophore Modeling.

Authors:  Martín Indarte; Yi Liu; Jeffry D Madura; Christopher K Surratt
Journal:  ACS Chem Neurosci       Date:  2010-03-17       Impact factor: 4.418

Review 3.  Monoamine transporter structure, function, dynamics, and drug discovery: a computational perspective.

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Journal:  AAPS J       Date:  2012-08-24       Impact factor: 4.009

4.  Lipophilic antifolate trimetrexate is a potent inhibitor of Trypanosoma cruzi: prospect for chemotherapy of Chagas' disease.

Authors:  Olga Senkovich; Vandanajay Bhatia; Nisha Garg; Debasish Chattopadhyay
Journal:  Antimicrob Agents Chemother       Date:  2005-08       Impact factor: 5.191

5.  Mild conditions for Pd-catalyzed carboamination of N-protected hex-4-enylamines and 1-, 3-, and 4-substituted pent-4-enylamines. Scope, limitations, and mechanism of pyrrolidine formation.

Authors:  Myra Beaudoin Bertrand; Joshua D Neukom; John P Wolfe
Journal:  J Org Chem       Date:  2008-10-23       Impact factor: 4.354

6.  Asymmetric [4 + 2] annulation of 5H-thiazol-4-ones with a chiral dipeptide-based Brønsted base catalyst.

Authors:  Bo Zhu; Shuai Qiu; Jiangtao Li; Michelle L Coote; Richmond Lee; Zhiyong Jiang
Journal:  Chem Sci       Date:  2016-06-09       Impact factor: 9.825
  6 in total

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