Literature DB >> 30108710

Novel lead compounds in pre-clinical development against African sleeping sickness.

Michael Berninger1, Ines Schmidt1, Alicia Ponte-Sucre2, Ulrike Holzgrabe1.   

Abstract

Human African trypanosomiasis (HAT), also known as African sleeping sickness, is caused by parasitic protozoa of the genus Trypanosoma. As the disease progresses, the parasites cross the blood brain barrier and are lethal for the patients if the disease is left untreated. Current therapies suffer from several drawbacks due to e.g. toxicity of the respective compounds or resistance to approved antitrypanosomal drugs. In this review, the different strategies of drug development against HAT are considered, namely the target-based approach, the phenotypic high throughput screening and the drug repurposing strategy. The most promising compounds emerging from these approaches entering an in vivo evaluation are mentioned herein. Of note, it may turn out to be difficult to confirm in vitro activity in an animal model of infection; however, possible reasons for the missing efficacy in unsuccessful in vivo studies are discussed.

Entities:  

Year:  2017        PMID: 30108710      PMCID: PMC6072528          DOI: 10.1039/c7md00280g

Source DB:  PubMed          Journal:  Medchemcomm        ISSN: 2040-2503            Impact factor:   3.597


  90 in total

1.  In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness.

Authors:  Tanja Wenzler; Sihyung Yang; Donald A Patrick; Olivier Braissant; Mohamed A Ismail; Richard R Tidwell; David W Boykin; Michael Zhuo Wang; Reto Brun
Journal:  Antimicrob Agents Chemother       Date:  2014-05-27       Impact factor: 5.191

2.  Pharmacokinetic comparison to determine the mechanisms underlying the differential efficacies of cationic diamidines against first- and second-stage human African trypanosomiasis.

Authors:  Sihyung Yang; Tanja Wenzler; Patrik N Miller; Huali Wu; David W Boykin; Reto Brun; Michael Zhuo Wang
Journal:  Antimicrob Agents Chemother       Date:  2014-05-05       Impact factor: 5.191

3.  Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites.

Authors:  Giuseppe Giannini; Gianfranco Battistuzzi
Journal:  Bioorg Med Chem Lett       Date:  2014-12-20       Impact factor: 2.823

4.  Novel bisnaphthalimidopropyl (BNIPs) derivatives as anticancer compounds targeting DNA in human breast cancer cells.

Authors:  Maria Kopsida; Gemma A Barron; Giovanna Bermano; Paul Kong Thoo Lin; Marie Goua
Journal:  Org Biomol Chem       Date:  2016-10-18       Impact factor: 3.876

5.  N-myristoyltransferase inhibitors as new leads to treat sleeping sickness.

Authors:  Julie A Frearson; Stephen Brand; Stuart P McElroy; Laura A T Cleghorn; Ondrej Smid; Laste Stojanovski; Helen P Price; M Lucia S Guther; Leah S Torrie; David A Robinson; Irene Hallyburton; Chidochangu P Mpamhanga; James A Brannigan; Anthony J Wilkinson; Michael Hodgkinson; Raymond Hui; Wei Qiu; Olawale G Raimi; Daan M F van Aalten; Ruth Brenk; Ian H Gilbert; Kevin D Read; Alan H Fairlamb; Michael A J Ferguson; Deborah F Smith; Paul G Wyatt
Journal:  Nature       Date:  2010-04-01       Impact factor: 49.962

6.  Synthesis and in vitro/in vivo evaluation of the antitrypanosomal activity of 3-bromoacivicin, a potent CTP synthetase inhibitor.

Authors:  Paola Conti; Andrea Pinto; Pui E Wong; Louise L Major; Lucia Tamborini; Maria C Iannuzzi; Carlo De Micheli; Michael P Barrett; Terry K Smith
Journal:  ChemMedChem       Date:  2010-12-22       Impact factor: 3.466

7.  Variant surface glycoproteins from Venezuelan trypanosome isolates are recognized by sera from animals infected with either Trypanosoma evansi or Trypanosoma vivax.

Authors:  Rocío Camargo; Adriana Izquier; Graciela L Uzcanga; Trina Perrone; Alvaro Acosta-Serrano; Liomary Carrasquel; Laura P Arias; José L Escalona; Vanessa Cardozo; José Bubis
Journal:  Vet Parasitol       Date:  2014-11-13       Impact factor: 2.738

Review 8.  Trypanosoma evansi and surra: a review and perspectives on transmission, epidemiology and control, impact, and zoonotic aspects.

Authors:  Marc Desquesnes; Alan Dargantes; De-Hua Lai; Zhao-Rong Lun; Philippe Holzmuller; Sathaporn Jittapalapong
Journal:  Biomed Res Int       Date:  2013-09-18       Impact factor: 3.411

9.  Erratum: Discovery of a Carbazole-Derived Lead Drug for Human African Trypanosomiasis.

Authors:  Sarah M Thomas; Andrei Purmal; Michael Pollastri; Kojo Mensa-Wilmot
Journal:  Sci Rep       Date:  2017-01-11       Impact factor: 4.379

10.  The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.

Authors:  Robert Urich; Raffaella Grimaldi; Torsten Luksch; Julie A Frearson; Ruth Brenk; Paul G Wyatt
Journal:  J Med Chem       Date:  2014-09-08       Impact factor: 7.446

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  7 in total

Review 1.  Trypanosoma brucei: Metabolomics for analysis of cellular metabolism and drug discovery.

Authors:  Fanta Fall; Lucia Mamede; Laura Schioppa; Allison Ledoux; Pascal De Tullio; Paul Michels; Michel Frédérich; Joëlle Quetin-Leclercq
Journal:  Metabolomics       Date:  2022-03-19       Impact factor: 4.290

2.  β-Sitosterol could serve as a dual inhibitor of Trypanosoma congolense sialidase and phospholipase A2: in vitro kinetic analyses and molecular dynamic simulations.

Authors:  Suleiman Aminu; Ammar Usman Danazumi; Zainab Aliyu Alhafiz; Maria Wiktoria Gorna; Mohammed Auwal Ibrahim
Journal:  Mol Divers       Date:  2022-08-30       Impact factor: 3.364

Review 3.  Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites.

Authors:  Magali Van den Kerkhof; Yann G-J Sterckx; Philippe Leprohon; Louis Maes; Guy Caljon
Journal:  Microorganisms       Date:  2020-06-24

4.  Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity.

Authors:  Maureen Gumbo; Richard M Beteck; Tawanda Mandizvo; Ronnett Seldon; Digby F Warner; Heinrich C Hoppe; Michelle Isaacs; Dustin Laming; Christina C Tam; Luisa W Cheng; Nicole Liu; Kirkwood M Land; Setshaba D Khanye
Journal:  Molecules       Date:  2018-08-15       Impact factor: 4.411

5.  Easy-To-Access Quinolone Derivatives Exhibiting Antibacterial and Anti-Parasitic Activities.

Authors:  Richard M Beteck; Audrey Jordaan; Ronnett Seldon; Dustin Laming; Heinrich C Hoppe; Digby F Warner; Setshaba D Khanye
Journal:  Molecules       Date:  2021-02-20       Impact factor: 4.411

Review 6.  Marine alkaloids as bioactive agents against protozoal neglected tropical diseases and malaria.

Authors:  Andre G Tempone; Pauline Pieper; Samanta E T Borborema; Fernanda Thevenard; Joao Henrique G Lago; Simon L Croft; Edward A Anderson
Journal:  Nat Prod Rep       Date:  2021-12-15       Impact factor: 13.423

7.  Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives.

Authors:  Ayanda I Zulu; Ogunyemi O Oderinlo; Cuan Kruger; Michelle Isaacs; Heinrich C Hoppe; Vincent J Smith; Clinton G L Veale; Setshaba D Khanye
Journal:  Molecules       Date:  2020-04-04       Impact factor: 4.411

  7 in total

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