Literature DB >> 23260352

Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold.

Claire-Lise Ciana1, Romain Siegrist, Hamed Aissaoui, Léo Marx, Sophie Racine, Solange Meyer, Christoph Binkert, Ruben de Kanter, Christoph Fischli, Sergio Wittlin, Christoph Boss.   

Abstract

A novel series of anti-malarials, based on a hydroxy-ethyl-amine scaffold, initially identified as peptidomimetic protease inhibitors is described. Combination of the hydroxy-ethyl-amine anti-malarial phramacophore with the known Mannich base pharmacophore of amodiaquine (57) resulted in promising in vivo active novel derivatives.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23260352     DOI: 10.1016/j.bmcl.2012.11.118

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  14 in total

Review 1.  Malaria medicines: a glass half full?

Authors:  Timothy N C Wells; Rob Hooft van Huijsduijnen; Wesley C Van Voorhis
Journal:  Nat Rev Drug Discov       Date:  2015-05-22       Impact factor: 84.694

2.  Evaluation of aminohydantoins as a novel class of antimalarial agents.

Authors:  Marvin J Meyers; Micky D Tortorella; Jing Xu; Limei Qin; Zhengxiang He; Xingfen Lang; Wentian Zeng; Wanwan Xu; Li Qin; Michael J Prinsen; Francis M Sverdrup; Christopher S Eickhoff; David W Griggs; Jonathan Oliva; Peter G Ruminski; E Jon Jacobsen; Mary A Campbell; David C Wood; Daniel E Goldberg; Xiaorong Liu; Yongzhi Lu; Xin Lu; Zhengchao Tu; Xiaoyun Lu; Ke Ding; Xiaoping Chen
Journal:  ACS Med Chem Lett       Date:  2013-12-06       Impact factor: 4.345

3.  Modeling and resistant alleles explain the selectivity of antimalarial compound 49c towards apicomplexan aspartyl proteases.

Authors:  Budhaditya Mukherjee; Francesca Tessaro; Juha Vahokoski; Inari Kursula; Jean-Baptiste Marq; Leonardo Scapozza; Dominique Soldati-Favre
Journal:  EMBO J       Date:  2018-03-08       Impact factor: 11.598

4.  Structures of plasmepsin II from Plasmodium falciparum in complex with two hydroxyethylamine-based inhibitors.

Authors:  Rosario Recacha; Janis Leitans; Inara Akopjana; Lilija Aprupe; Peteris Trapencieris; Kristaps Jaudzems; Aigars Jirgensons; Kaspars Tars
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2015-11-27       Impact factor: 1.056

5.  Evaluation of spiropiperidine hydantoins as a novel class of antimalarial agents.

Authors:  Marvin J Meyers; Elizabeth J Anderson; Sarah A McNitt; Thomas M Krenning; Megh Singh; Jing Xu; Wentian Zeng; Limei Qin; Wanwan Xu; Siting Zhao; Li Qin; Christopher S Eickhoff; Jonathan Oliva; Mary A Campbell; Stacy D Arnett; Michael J Prinsen; David W Griggs; Peter G Ruminski; Daniel E Goldberg; Ke Ding; Xiaorong Liu; Zhengchao Tu; Micky D Tortorella; Francis M Sverdrup; Xiaoping Chen
Journal:  Bioorg Med Chem       Date:  2015-03-04       Impact factor: 3.641

Review 6.  New insight-guided approaches to detect, cure, prevent and eliminate malaria.

Authors:  Sushil Kumar; Renu Kumari; Richa Pandey
Journal:  Protoplasma       Date:  2014-10-17       Impact factor: 3.356

7.  Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit.

Authors:  Kristaps Jaudzems; Kaspars Tars; Gundars Maurops; Natalija Ivdra; Martins Otikovs; Janis Leitans; Iveta Kanepe-Lapsa; Ilona Domraceva; Ilze Mutule; Peteris Trapencieris; Michael J Blackman; Aigars Jirgensons
Journal:  ACS Med Chem Lett       Date:  2014-01-13       Impact factor: 4.345

Review 8.  Mannich bases in medicinal chemistry and drug design.

Authors:  Gheorghe Roman
Journal:  Eur J Med Chem       Date:  2014-10-30       Impact factor: 6.514

9.  Structures of plasmepsin X from Plasmodium falciparum reveal a novel inactivation mechanism of the zymogen and molecular basis for binding of inhibitors in mature enzyme.

Authors:  Pooja Kesari; Anuradha Deshmukh; Nikhil Pahelkar; Abhishek B Suryawanshi; Ishan Rathore; Vandana Mishra; John H Dupuis; Huogen Xiao; Alla Gustchina; Jan Abendroth; Mehdi Labaied; Rickey Y Yada; Alexander Wlodawer; Thomas E Edwards; Donald D Lorimer; Prasenjit Bhaumik
Journal:  Protein Sci       Date:  2022-02-05       Impact factor: 6.725

10.  A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress.

Authors:  Paco Pino; Reto Caldelari; Budhaditya Mukherjee; Juha Vahokoski; Natacha Klages; Bohumil Maco; Christine R Collins; Michael J Blackman; Inari Kursula; Volker Heussler; Mathieu Brochet; Dominique Soldati-Favre
Journal:  Science       Date:  2017-10-27       Impact factor: 47.728

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