Literature DB >> 22018462

Identification of small-molecule inhibitors of Trypansoma cruzi replication.

Andrew R Germain1, Leigh C Carmody, Chris Dockendorff, Cristina Galan-Rodriguez, Ana Rodriguez, Stephen Johnston, Joshua A Bittker, Lawrence MacPherson, Sivaraman Dandapani, Michelle Palmer, Stuart L Schreiber, Benito Munoz.   

Abstract

We report the outcome of a high-throughput small-molecule screen to identify novel, nontoxic, inhibitors of Trypansoma cruzi, as potential starting points for therapeutics to treat for both the acute and chronic stages of Chagas disease. Two compounds were identified that displayed nanomolar inhibition of T. cruzi and an absence of activity against host cells at the highest tested dose. These compounds have been registered with NIH Molecular Libraries Program (probes ML157 and ML158). Copyright Â
© 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22018462     DOI： 10.1016/j.bmcl.2011.09.057

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


  5 in total

1.  Identification of Piperidine-3-carboxamide Derivatives Inducing Senescence-like Phenotype with Antimelanoma Activities.

Authors:  Sangmi Oh; Do Yoon Kwon; Inhee Choi; Young Mi Kim; Ji Young Lee; Jiyoung Ryu; Hangyeol Jeong; Myung Jin Kim; Rita Song
Journal:  ACS Med Chem Lett       Date:  2021-03-22       Impact factor: 4.345

2.  Machine Learning Models and Pathway Genome Data Base for Trypanosoma cruzi Drug Discovery.

Authors:  Sean Ekins; Jair Lage de Siqueira-Neto; Laura-Isobel McCall; Malabika Sarker; Maneesh Yadav; Elizabeth L Ponder; E Adam Kallel; Danielle Kellar; Steven Chen; Michelle Arkin; Barry A Bunin; James H McKerrow; Carolyn Talcott
Journal:  PLoS Negl Trop Dis       Date:  2015-06-26

Review 3.  High throughput screening for anti-Trypanosoma cruzi drug discovery.

Authors:  Julio Alonso-Padilla; Ana Rodríguez
Journal:  PLoS Negl Trop Dis       Date:  2014-12-04

4.  Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.

Authors:  Stephen Brand; Eun Jung Ko; Elisabet Viayna; Stephen Thompson; Daniel Spinks; Michael Thomas; Lars Sandberg; Amanda F Francisco; Shiromani Jayawardhana; Victoria C Smith; Chimed Jansen; Manu De Rycker; John Thomas; Lorna MacLean; Maria Osuna-Cabello; Jennifer Riley; Paul Scullion; Laste Stojanovski; Frederick R C Simeons; Ola Epemolu; Yoko Shishikura; Sabrinia D Crouch; Tania S Bakshi; Christopher J Nixon; Iain H Reid; Alan P Hill; Tim Z Underwood; Sean J Hindley; Sharon A Robinson; John M Kelly; Jose M Fiandor; Paul G Wyatt; Maria Marco; Timothy J Miles; Kevin D Read; Ian H Gilbert
Journal:  J Med Chem       Date:  2017-08-27       Impact factor: 7.446

Review 5.  Kinases as druggable targets in trypanosomatid protozoan parasites.

Authors:  Christopher Merritt; Lisseth E Silva; Angela L Tanner; Kenneth Stuart; Michael P Pollastri
Journal:  Chem Rev       Date:  2014-10-07       Impact factor: 60.622
  5 in total

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