Literature DB >> 30174152

Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).

Denise J Tsagris1, Kristian Birchall2, Nathalie Bouloc2, Jonathan M Large2, Andy Merritt2, Ela Smiljanic-Hurley2, Mary Wheldon2, Keith H Ansell2, Catherine Kettleborough2, David Whalley2, Lindsay B Stewart3, Paul W Bowyer3, David A Baker3, Simon A Osborne2.   

Abstract

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Malaria; PfPKG; Plasmodium falciparum; Thiazole

Mesh：

Substances：

Year:  2018        PMID： 30174152      PMCID： PMC6193536          DOI： 10.1016/j.bmcl.2018.08.028

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


  13 in total

1.  Anticoccidial kinase inhibitors: identification of protein kinase targets secondary to cGMP-dependent protein kinase.

Authors:  Robert G K Donald; Tanya Zhong; Helen Wiersma; Bakela Nare; Dan Yao; Anita Lee; John Allocco; Paul A Liberator
Journal:  Mol Biochem Parasitol       Date:  2006-05-23       Impact factor: 1.759

2.  Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents.

Authors:  Tesfaye Biftu; Dennis Feng; Michael Fisher; Gui-Bai Liang; Xiaoxia Qian; Andrew Scribner; Richard Dennis; Shuliang Lee; Paul A Liberator; Chris Brown; Anne Gurnett; Penny S Leavitt; Donald Thompson; John Mathew; Andrew Misura; Samantha Samaras; Tamas Tamas; Joseph F Sina; Kathleen A McNulty; Crystal G McKnight; Dennis M Schmatz; Matthew Wyvratt
Journal:  Bioorg Med Chem Lett       Date:  2006-02-07       Impact factor: 2.823

3.  The threat of artemisinin-resistant malaria.

Authors:  Arjen M Dondorp; Rick M Fairhurst; Laurence Slutsker; John R Macarthur; Joel G Breman; Philippe J Guerin; Thomas E Wellems; Pascal Ringwald; Robert D Newman; Christopher V Plowe
Journal:  N Engl J Med       Date:  2011-09-22       Impact factor: 91.245

4.  Purification and molecular characterization of cGMP-dependent protein kinase from Apicomplexan parasites. A novel chemotherapeutic target.

Authors:  Anne M Gurnett; Paul A Liberator; Paula M Dulski; Scott P Salowe; Robert G K Donald; Jennifer W Anderson; Judyann Wiltsie; Carmen A Diaz; Georgiana Harris; Ben Chang; Sandra J Darkin-Rattray; Bakela Nare; Tami Crumley; Penny Sue Blum; Andrew S Misura; Tamas Tamas; Mohinder K Sardana; Jeffrey Yuan; Tesfaye Biftu; Dennis M Schmatz
Journal:  J Biol Chem       Date:  2002-02-07       Impact factor: 5.157

5.  Kinase selectivity potential for inhibitors targeting the ATP binding site: a network analysis.

Authors:  Danzhi Huang; Ting Zhou; Karine Lafleur; Cristina Nevado; Amedeo Caflisch
Journal:  Bioinformatics       Date:  2009-11-26       Impact factor: 6.937

6.  Role of Plasmodium berghei cGMP-dependent protein kinase in late liver stage development.

Authors:  Adebola Falae; Audrey Combe; Anburaj Amaladoss; Teresa Carvalho; Robert Menard; Purnima Bhanot
Journal:  J Biol Chem       Date:  2009-11-24       Impact factor: 5.157

7.  Phosphoproteomics reveals malaria parasite Protein Kinase G as a signalling hub regulating egress and invasion.

Authors:  Mahmood M Alam; Lev Solyakov; Andrew R Bottrill; Christian Flueck; Faiza A Siddiqui; Shailja Singh; Sharad Mistry; Maria Viskaduraki; Kate Lee; Christine S Hopp; Chetan E Chitnis; Christian Doerig; Robert W Moon; Judith L Green; Anthony A Holder; David A Baker; Andrew B Tobin
Journal:  Nat Commun       Date:  2015-07-07       Impact factor: 14.919

8.  A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.

Authors:  David A Baker; Lindsay B Stewart; Jonathan M Large; Paul W Bowyer; Keith H Ansell; María B Jiménez-Díaz; Majida El Bakkouri; Kristian Birchall; Koen J Dechering; Nathalie S Bouloc; Peter J Coombs; David Whalley; Denise J Harding; Ela Smiljanic-Hurley; Mary C Wheldon; Eloise M Walker; Johannes T Dessens; María José Lafuente; Laura M Sanz; Francisco-Javier Gamo; Santiago B Ferrer; Raymond Hui; Teun Bousema; Iñigo Angulo-Barturén; Andy T Merritt; Simon L Croft; Winston E Gutteridge; Catherine A Kettleborough; Simon A Osborne
Journal:  Nat Commun       Date:  2017-09-05       Impact factor: 14.919

9.  Invasion of hepatocytes by Plasmodium sporozoites requires cGMP-dependent protein kinase and calcium dependent protein kinase 4.

Authors:  K Govindasamy; S Jebiwott; D K Jaijyan; A Davidow; K K Ojo; W C Van Voorhis; M Brochet; O Billker; P Bhanot
Journal:  Mol Microbiol       Date:  2016-08-09       Impact factor: 3.501

10.  Gametogenesis in malaria parasites is mediated by the cGMP-dependent protein kinase.

Authors:  Louisa McRobert; Cathy J Taylor; Wensheng Deng; Quinton L Fivelman; Ross M Cummings; Spencer D Polley; Oliver Billker; David A Baker
Journal:  PLoS Biol       Date:  2008-06-03       Impact factor: 8.029
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  10 in total

1.  Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase.

Authors:  Shams Ul Mahmood; Huimin Cheng; Sreedhar R Tummalapalli; Ramappa Chakrasali; Rammohan R Yadav Bheemanaboina; Tamara Kreiss; Agnieska Chojnowski; Tyler Eck; John J Siekierka; David P Rotella
Journal:  RSC Med Chem       Date:  2019-12-16

2.  Physicochemical Profiling and Comparison of Research Antiplasmodials and Advanced Stage Antimalarials with Oral Drugs.

Authors:  Amritansh Bhanot; Sandeep Sundriyal
Journal:  ACS Omega       Date:  2021-02-25

3.  Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.

Authors:  Tyler Eck; Mariana Laureano de Souza; Melvin Delvillar; Kutub Ashraf; Rammohan R Yadav Bheemanaboina; Ramappa Chakrasali; Tamara Kreiss; John J Siekierka; David P Rotella; Purnima Bhanot; Nina M Goodey
Journal:  Chembiochem       Date:  2022-02-23       Impact factor: 3.461

4.  High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage parasites.

Authors:  Maria Penzo; Laura de Las Heras-Dueña; Lydia Mata-Cantero; Beatriz Diaz-Hernandez; Maria-Jesus Vazquez-Muñiz; Sonja Ghidelli-Disse; Gerard Drewes; Elena Fernandez-Alvaro; David A Baker
Journal:  Sci Rep       Date:  2019-05-07       Impact factor: 4.379

5.  Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines.

Authors:  Jonathan M Large; Kristian Birchall; Nathalie S Bouloc; Andy T Merritt; Ela Smiljanic-Hurley; Denise J Tsagris; Mary C Wheldon; Keith H Ansell; Peter J Coombs; Catherine A Kettleborough; David Whalley; Lindsay B Stewart; Paul W Bowyer; David A Baker; Simon A Osborne
Journal:  Bioorg Med Chem Lett       Date:  2018-11-20       Impact factor: 2.823

6.  An enhanced toolkit for the generation of knockout and marker-free fluorescent Plasmodium chabaudi.

Authors:  Edward J Marr; Rachel M Milne; Burcu Anar; Gareth Girling; Frank Schwach; Jason P Mooney; Wiebke Nahrendorf; Philip J Spence; Deirdre Cunningham; David A Baker; Jean Langhorne; Julian C Rayner; Oliver Billker; Ellen S Bushell; Joanne Thompson
Journal:  Wellcome Open Res       Date:  2020-06-24

7.  Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty.

Authors:  Jonathan M Large; Kristian Birchall; Nathalie S Bouloc; Andy T Merritt; Ela Smiljanic-Hurley; Denise J Tsagris; Mary C Wheldon; Keith H Ansell; Peter J Coombs; Catherine A Kettleborough; David Whalley; Lindsay B Stewart; Paul W Bowyer; David A Baker; Simon A Osborne
Journal:  Bioorg Med Chem Lett       Date:  2019-08-09       Impact factor: 2.823

Review 8.  Plasmodium Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities.

Authors:  Lauren B Arendse; Susan Wyllie; Kelly Chibale; Ian H Gilbert
Journal:  ACS Infect Dis       Date:  2021-02-16       Impact factor: 5.084

9.  Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites.

Authors:  Alexios N Matralis; Adnan Malik; Maria Penzo; Inmaculada Moreno; Maria J Almela; Isabel Camino; Benigno Crespo; Anas Saadeddin; Sonja Ghidelli-Disse; Lourdes Rueda; Felix Calderon; Simon A Osborne; Gerard Drewes; Markus Böesche; Elena Fernández-Álvaro; Jose Ignacio Martin Hernando; David A Baker
Journal:  J Med Chem       Date:  2019-10-14       Impact factor: 7.446

Review 10.  An Update on Development of Small-Molecule Plasmodial Kinase Inhibitors.

Authors:  Chantalle Moolman; Rencia van der Sluis; Richard M Beteck; Lesetja J Legoabe
Journal:  Molecules       Date:  2020-11-07       Impact factor: 4.411
  10 in total

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