Literature DB >> 32184953

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

Baljinder Singh1, Jean A Bernatchez2, Laura-Isobel McCall2, Claudia M Calvet2, Jasmin Ackermann2, Julia M Souza2, Diane Thomas2, Everton M Silva2, Kelly A Bachovchin1, Dana M Klug1, Hitesh B Jalani1, Seema Bag1, Melissa J Buskes1, Susan E Leed3, Norma E Roncal3, Erica C Penn3, Jessey Erath4, Ana Rodriguez4, Richard J Sciotti3, Robert F Campbell3, James McKerrow2, Jair L Siqueira-Neto2, Lori Ferrins1, Michael P Pollastri1.   

Abstract

Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.
Copyright © 2020 American Chemical Society.

Entities:  

Year:  2020        PMID： 32184953      PMCID： PMC7073875          DOI： 10.1021/acsmedchemlett.9b00453

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  12 in total

Review 1.  Emerging and reemerging neglected tropical diseases: a review of key characteristics, risk factors, and the policy and innovation environment.

Authors:  Tim K Mackey; Bryan A Liang; Raphael Cuomo; Ryan Hafen; Kimberly C Brouwer; Daniel E Lee
Journal:  Clin Microbiol Rev       Date:  2014-10       Impact factor: 26.132

Review 2.  Hit and lead criteria in drug discovery for infectious diseases of the developing world.

Authors:  Kei Katsuno; Jeremy N Burrows; Ken Duncan; Rob Hooft van Huijsduijnen; Takushi Kaneko; Kiyoshi Kita; Charles E Mowbray; Dennis Schmatz; Peter Warner; B T Slingsby
Journal:  Nat Rev Drug Discov       Date:  2015-10-05       Impact factor: 84.694

Review 3.  Repurposing strategies for tropical disease drug discovery.

Authors:  Dana M Klug; Michael H Gelb; Michael P Pollastri
Journal:  Bioorg Med Chem Lett       Date:  2016-03-30       Impact factor: 2.823

Review 4.  Leishmaniasis drug discovery: recent progress and challenges in assay development.

Authors:  Bilal Zulfiqar; Todd B Shelper; Vicky M Avery
Journal:  Drug Discov Today       Date:  2017-06-21       Impact factor: 7.851

Review 5.  Chagas Cardiomyopathy in Latin America Review.

Authors:  Jefferson Luis Vieira; Fábio Rocha Fernandes Távora; Maria Gyslane Vasconcelos Sobral; Glauber Gean Vasconcelos; Germana Porto Linhares Almeida; Juliana Rolim Fernandes; Laura Leite da Escóssia Marinho; Daniel Francisco de Mendonça Trompieri; João David De Souza Neto; Juan Alberto Cosquillo Mejia
Journal:  Curr Cardiol Rep       Date:  2019-02-12       Impact factor: 3.955

Review 6.  Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Authors:  Mark C Field; David Horn; Alan H Fairlamb; Michael A J Ferguson; David W Gray; Kevin D Read; Manu De Rycker; Leah S Torrie; Paul G Wyatt; Susan Wyllie; Ian H Gilbert
Journal:  Nat Rev Microbiol       Date:  2017-02-27       Impact factor: 60.633

7.  Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery.

Authors:  William Devine; Jennifer L Woodring; Uma Swaminathan; Emanuele Amata; Gautam Patel; Jessey Erath; Norma E Roncal; Patricia J Lee; Susan E Leed; Ana Rodriguez; Kojo Mensa-Wilmot; Richard J Sciotti; Michael P Pollastri
Journal:  J Med Chem       Date:  2015-07-08       Impact factor: 7.446

8.  Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.

Authors:  William Devine; Sarah M Thomas; Jessey Erath; Kelly A Bachovchin; Patricia J Lee; Susan E Leed; Ana Rodriguez; Richard J Sciotti; Kojo Mensa-Wilmot; Michael P Pollastri
Journal:  ACS Med Chem Lett       Date:  2017-02-05       Impact factor: 4.345

9.  Anilinoquinoline based inhibitors of trypanosomatid proliferation.

Authors:  Lori Ferrins; Amrita Sharma; Sarah M Thomas; Naimee Mehta; Jessey Erath; Scott Tanghe; Susan E Leed; Ana Rodriguez; Kojo Mensa-Wilmot; Richard J Sciotti; Kirsten Gillingwater; Michael P Pollastri
Journal:  PLoS Negl Trop Dis       Date:  2018-11-26

Review 10.  Heart failure in South America.

Authors:  Edimar Alcides Bocchi
Journal:  Curr Cardiol Rev       Date:  2013-05
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  4 in total

1.  Structure-property studies of an imidazoquinoline chemotype with antitrypanosomal activity.

Authors:  Dana M Klug; Rosario Diaz-Gonzalez; Travis J DeLano; Eftychia M Mavrogiannaki; Melissa J Buskes; Raeann M Dalton; John K Fisher; Katherine M Schneider; Vivian Hilborne; Melanie G Fritsche; Quillon J Simpson; Westley F Tear; William G Devine; Guiomar Pérez-Moreno; Gloria Ceballos-Pérez; Raquel García-Hernández; Cristina Bosch-Navarrete; Luis Miguel Ruiz-Pérez; Francisco Gamarro; Dolores González-Pacanowska; Maria Santos Martinez-Martinez; Pilar Manzano-Chinchon; Miguel Navarro; Michael P Pollastri; Lori Ferrins
Journal:  RSC Med Chem       Date:  2020-07-10

2.  Identification of Leucinostatins from Ophiocordyceps sp. as Antiparasitic Agents against Trypanosoma cruzi.

Authors:  Jean A Bernatchez; Yun-Seo Kil; Elany Barbosa da Silva; Diane Thomas; Laura-Isobel McCall; Karen L Wendt; Julia M Souza; Jasmin Ackermann; James H McKerrow; Robert H Cichewicz; Jair L Siqueira-Neto
Journal:  ACS Omega       Date:  2022-01-28

3.  Collaborative virtual screening to elaborate an imidazo[1,2-a]pyridine hit series for visceral leishmaniasis.

Authors:  Yuichiro Akao; Stacie Canan; Yafeng Cao; Kevin Condroski; Ola Engkvist; Sachiko Itono; Rina Kaki; Chiaki Kimura; Thierry Kogej; Kazuya Nagaoka; Akira Naito; Hiromi Nakai; Garry Pairaudeau; Constantin Radu; Ieuan Roberts; Mitsuyuki Shimada; David Shum; Nao-Aki Watanabe; Huanxu Xie; Shuji Yonezawa; Osamu Yoshida; Ryu Yoshida; Charles Mowbray; Benjamin Perry
Journal:  RSC Med Chem       Date:  2021-01-21

4.  Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis.

Authors:  Dana M Klug; Eftychia M Mavrogiannaki; Katherine C Forbes; Lisseth Silva; Rosario Diaz-Gonzalez; Guiomar Pérez-Moreno; Gloria Ceballos-Pérez; Raquel Garcia-Hernández; Cristina Bosch-Navarrete; Carlos Cordón-Obras; Claudia Gómez-Liñán; Andreu Saura; Jeremiah D Momper; Maria Santos Martinez-Martinez; Pilar Manzano; Ali Syed; Nelly El-Sakkary; Conor R Caffrey; Francisco Gamarro; Luis Miguel Ruiz-Perez; Dolores Gonzalez Pacanowska; Lori Ferrins; Miguel Navarro; Michael P Pollastri
Journal:  J Med Chem       Date:  2021-06-22       Impact factor: 8.039
  4 in total

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