Literature DB >> 24530464

N¹,N¹-Dimethyl-N³-(3-(trifluoromethyl)phenethyl)propane-1,3-diamine, a new lead for the treatment of human African trypanosomiasis.

Ngoc B Pham1, Sophie Deydier1, Mehdi Labaied2, Séverine Monnerat2, Kenneth Stuart2, Ronald J Quinn3.   

Abstract

The natural product, convolutamine I (1), has anti-trypanosomal activity however it has a high molecular weight of 473 due to a presence of 3 bromine atoms. The synthesis of the natural product convolutamine I (1) together with its analogues are presented. A SAR study against Trypanosoma brucei brucei led to compounds with improved physico-chemical properties: lower molecular weight and lower log P while maintaining potency (with a slight 2-fold improvement).
Copyright © 2014 The Authors. Published by Elsevier Masson SAS.. All rights reserved.

Entities:  

Keywords:  Alkaloids; Anti-parasite; Anti-protozoa; Human African trypanosomiasis

Mesh：

Substances：

Year:  2014        PMID： 24530464      PMCID： PMC4296322          DOI： 10.1016/j.ejmech.2013.12.050

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


  7 in total

1.  Development of an Alamar Blue viability assay in 384-well format for high throughput whole cell screening of Trypanosoma brucei brucei bloodstream form strain 427.

Authors:  Melissa L Sykes; Vicky M Avery
Journal:  Am J Trop Med Hyg       Date:  2009-10       Impact factor: 2.345

2.  Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa.

Authors:  Rohan A Davis; Melissa Sykes; Vicky M Avery; David Camp; Ronald J Quinn
Journal:  Bioorg Med Chem       Date:  2011-06-12       Impact factor: 3.641

3.  Fluorine in medicinal chemistry: a century of progress and a 60-year retrospective of selected highlights.

Authors:  Robert Filler; Rituparna Saha
Journal:  Future Med Chem       Date:  2009-08       Impact factor: 3.808

4.  Cesium effect: high chemoselectivity in direct N-alkylation of amines.

Authors:  Ralph Nicholas Salvatore; Advait S Nagle; Kyung Woon Jung
Journal:  J Org Chem       Date:  2002-02-08       Impact factor: 4.354

5.  Nifurtimox-eflornithine combination therapy for second-stage gambiense human African trypanosomiasis: Médecins Sans Frontières experience in the Democratic Republic of the Congo.

Authors:  Emilie Alirol; David Schrumpf; Josué Amici Heradi; Andrea Riedel; Catherine de Patoul; Michel Quere; François Chappuis
Journal:  Clin Infect Dis       Date:  2012-10-16       Impact factor: 9.079

Review 6.  Medicinal chemical properties of successful central nervous system drugs.

Authors:  Hassan Pajouhesh; George R Lenz
Journal:  NeuroRx       Date:  2005-10

7.  Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery.

Authors:  Arup K Ghose; Torsten Herbertz; Robert L Hudkins; Bruce D Dorsey; John P Mallamo
Journal:  ACS Chem Neurosci       Date:  2011-11-02       Impact factor: 4.418
  7 in total
  2 in total

Review 1.  Recent Advances in the Discovery of Novel Antiprotozoal Agents.

Authors:  Seong-Min Lee; Min-Sun Kim; Faisal Hayat; Dongyun Shin
Journal:  Molecules       Date:  2019-10-28       Impact factor: 4.411

Review 2.  The Phylum Bryozoa: From Biology to Biomedical Potential.

Authors:  Maria Letizia Ciavatta; Florence Lefranc; Leandro M Vieira; Robert Kiss; Marianna Carbone; Willem A L van Otterlo; Nicole B Lopanik; Andrea Waeschenbach
Journal:  Mar Drugs       Date:  2020-04-09       Impact factor: 5.118
  2 in total

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