Literature DB >> 29701144

Current and Future Prospects of Nitro-compounds as Drugs for Trypanosomiasis and Leishmaniasis.

Stephen Patterson1, Alan H Fairlamb1.   

Abstract

Interest in nitroheterocyclic drugs for the treatment of infectious diseases has undergone a resurgence in recent years. Here we review the current status of monocyclic and bicyclic nitroheterocyclic compounds as existing or potential new treatments for visceral leishmaniasis, Chagas' disease and human African trypanosomiasis. Both monocyclic (nifurtimox, benznidazole and fexinidazole) and bicyclic (pretomanid (PA-824) and delamanid (OPC-67683)) nitro-compounds are prodrugs, requiring enzymatic activation to exert their parasite toxicity. Current understanding of the nitroreductases involved in activation and possible mechanisms by which parasites develop resistance is discussed along with a description of the pharmacokinetic / pharmacodynamic behaviour and chemical structure-activity relationships of drugs and experimental compounds. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Entities:  

Keywords:  Chagas' disease; Human African trypanosomiasis; benznidazole; delamanid; fexinidazole; nifurtimox; nitro-drugs; pretomanid; visceral leishmaniasis.

Mesh:

Substances:

Year:  2019        PMID: 29701144     DOI: 10.2174/0929867325666180426164352

Source DB:  PubMed          Journal:  Curr Med Chem        ISSN: 0929-8673            Impact factor:   4.530


  12 in total

1.  Vinyl sulfone-based inhibitors of trypanosomal cysteine protease rhodesain with improved antitrypanosomal activities.

Authors:  Huaisheng Zhang; Jasmine Collins; Rogers Nyamwihura; Olamide Crown; Oluwatomi Ajayi; Ifedayo Victor Ogungbe
Journal:  Bioorg Med Chem Lett       Date:  2020-04-28       Impact factor: 2.823

2.  Screening and Identification of Metacaspase Inhibitors: Evaluation of Inhibition Mechanism and Trypanocidal Activity.

Authors:  Brian Pérez; León A Bouvier; Juan José Cazzulo; Fernán Agüero; Emir Salas-Sarduy; Vanina E Alvarez
Journal:  Antimicrob Agents Chemother       Date:  2021-02-17       Impact factor: 5.191

3.  Nongenotoxic 3-Nitroimidazo[1,2-a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity.

Authors:  Cyril Fersing; Louise Basmaciyan; Clotilde Boudot; Julien Pedron; Sébastien Hutter; Anita Cohen; Caroline Castera-Ducros; Nicolas Primas; Michèle Laget; Magali Casanova; Sandra Bourgeade-Delmas; Mélanie Piednoel; Alix Sournia-Saquet; Valère Belle Mbou; Bertrand Courtioux; Élisa Boutet-Robinet; Marc Since; Rachel Milne; Susan Wyllie; Alan H Fairlamb; Alexis Valentin; Pascal Rathelot; Pierre Verhaeghe; Patrice Vanelle; Nadine Azas
Journal:  ACS Med Chem Lett       Date:  2018-12-19       Impact factor: 4.345

4.  Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity.

Authors:  Juliana da Silva Pacheco; Débora de Souza Costa; Edézio Ferreira Cunha-Júnior; Valter Viana Andrade-Neto; Alan H Fairlamb; Susan Wyllie; Marília O F Goulart; Danyelle C Santos; Thaissa L Silva; Marina A Alves; Paulo R R Costa; Ayres G Dias; Eduardo Caio Torres-Santos
Journal:  ACS Med Chem Lett       Date:  2021-08-16       Impact factor: 4.632

Review 5.  Recent Progress in the Synthesis of Drugs and Bioactive Molecules Incorporating Nitro(het)arene Core.

Authors:  Maxim Bastrakov; Alexey Starosotnikov
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-03

6.  Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions.

Authors:  Julien Pedron; Clotilde Boudot; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Lucie Paloque; Maryam Rastegari; Mansour Abdoulaye; Hussein El-Kashef; Colin Bonduelle; Geneviève Pratviel; Susan Wyllie; Alan H Fairlamb; Bertrand Courtioux; Pierre Verhaeghe; Alexis Valentin
Journal:  ChemMedChem       Date:  2018-09-17       Impact factor: 3.466

7.  Novel benzoxaborole, nitroimidazole and aminopyrazoles with activity against experimental cutaneous leishmaniasis.

Authors:  Katrien Van Bocxlaer; Diana Caridha; Chad Black; Brian Vesely; Susan Leed; Richard J Sciotti; Gert-Jan Wijnant; Vanessa Yardley; Stéphanie Braillard; Charles E Mowbray; Jean-Robert Ioset; Simon L Croft
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2019-02-26       Impact factor: 4.077

8.  Antileishmanial assessment of isoxazole derivatives against L. donovani.

Authors:  Sushobhan Mukhopadhyay; Dinesh S Barak; R Karthik; Sarvesh K Verma; Rabi S Bhatta; Neena Goyal; Sanjay Batra
Journal:  RSC Med Chem       Date:  2020-07-20

Review 9.  Challenges in Chagas Disease Drug Development.

Authors:  Amanda F Francisco; Shiromani Jayawardhana; Francisco Olmo; Michael D Lewis; Shane R Wilkinson; Martin C Taylor; John M Kelly
Journal:  Molecules       Date:  2020-06-17       Impact factor: 4.411

10.  New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.

Authors:  Julien Pedron; Clotilde Boudot; Jean-Yves Brossas; Emilie Pinault; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Elisa Boutet-Robinet; Alexandre Destere; Antoine Tronnet; Justine Bergé; Colin Bonduelle; Céline Deraeve; Geneviève Pratviel; Jean-Luc Stigliani; Luc Paris; Dominique Mazier; Sophie Corvaisier; Marc Since; Aurélie Malzert-Fréon; Susan Wyllie; Rachel Milne; Alan H Fairlamb; Alexis Valentin; Bertrand Courtioux; Pierre Verhaeghe
Journal:  ACS Med Chem Lett       Date:  2020-02-06       Impact factor: 4.345

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