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Literature DB >> 27780638

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.

Wenlin Huang¹, Matthew A Hulverson², Zhongsheng Zhang¹, Ryan Choi², Kevin J Hart³, Mark Kennedy³, Rama Subba Rao Vidadala⁴, Dustin J Maly⁵, Wesley C Van Voorhis⁶, Scott E Lindner³, Erkang Fan⁷, Kayode K Ojo⁸.

Abstract

Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.

Entities: CellLine Chemical Disease Gene Mutation Species

Keywords: 5-Aminopyrazole-4-carboxamide; Malaria transmission blocking; Microgametocyte exflagellation; PfCDPK4; Plasmodium falciparum

Mesh：

Substances：

Year: 2016 PMID： 27780638 PMCID： PMC5159281 DOI： 10.1016/j.bmcl.2016.10.014

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

18 in total

1. The gatekeeper residue and beyond: homologous calcium-dependent protein kinases as drug development targets for veterinarian Apicomplexa parasites.

Authors: Katelyn R Keyloun; Molly C Reid; Ryan Choi; Yifan Song; Anna M W Fox; Heidi K Hillesland; Zhongsheng Zhang; RamaSubbaRao Vidadala; Ethan A Merritt; Audrey O T Lau; Dustin J Maly; Erkang Fan; Lynn K Barrett; Wesley C Van Voorhis; Kayode K Ojo
Journal: Parasitology Date: 2014-06-13 Impact factor: 3.234

2. Primaquine: report from CDC expert meeting on malaria chemoprophylaxis I.

Authors: David R Hill; J Kevin Baird; Monica E Parise; Linda S Lewis; Edward T Ryan; Alan J Magill
Journal: Am J Trop Med Hyg Date: 2006-09 Impact factor: 2.345

3. Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.

Authors: Ryan C Murphy; Kayode K Ojo; Eric T Larson; Alejandro Castellanos-Gonzalez; B Gayani K Perera; Katelyn R Keyloun; Jessica E Kim; Janhavi G Bhandari; Natascha R Muller; Christophe L M J Verlinde; A Clinton White; Ethan A Merritt; Wesley C Van Voorhis; Dustin J Maly
Journal: ACS Med Chem Lett Date: 2010-10-14 Impact factor: 4.345

4. The global distribution of clinical episodes of Plasmodium falciparum malaria.

Authors: Robert W Snow; Carlos A Guerra; Abdisalan M Noor; Hla Y Myint; Simon I Hay
Journal: Nature Date: 2005-03-10 Impact factor: 49.962

5. Transmission of malaria to mosquitoes blocked by bumped kinase inhibitors.

Authors: Kayode K Ojo; Claudia Pfander; Natascha R Mueller; Charlotte Burstroem; Eric T Larson; Cassie M Bryan; Anna M W Fox; Molly C Reid; Steven M Johnson; Ryan C Murphy; Mark Kennedy; Henning Mann; David J Leibly; Stephen N Hewitt; Christophe L M J Verlinde; Stefan Kappe; Ethan A Merritt; Dustin J Maly; Oliver Billker; Wesley C Van Voorhis
Journal: J Clin Invest Date: 2012-05-08 Impact factor: 14.808

6. Development of potent and selective Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) inhibitors that block the transmission of malaria to mosquitoes.

Authors: Rama Subba Rao Vidadala; Kayode K Ojo; Steven M Johnson; Zhongsheng Zhang; Stephen E Leonard; Arinjay Mitra; Ryan Choi; Molly C Reid; Katelyn R Keyloun; Anna M W Fox; Mark Kennedy; Tiffany Silver-Brace; Jen C C Hume; Stefan Kappe; Christophe L M J Verlinde; Erkang Fan; Ethan A Merritt; Wesley C Van Voorhis; Dustin J Maly
Journal: Eur J Med Chem Date: 2014-01-11 Impact factor: 6.514

7. Imidazopyridazine Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 Also Target Cyclic GMP-Dependent Protein Kinase and Heat Shock Protein 90 To Kill the Parasite at Different Stages of Intracellular Development.

Authors: Judith L Green; Robert W Moon; David Whalley; Paul W Bowyer; Claire Wallace; Ankit Rochani; Rishi K Nageshan; Steven A Howell; Munira Grainger; Hayley M Jones; Keith H Ansell; Timothy M Chapman; Debra L Taylor; Simon A Osborne; David A Baker; Utpal Tatu; Anthony A Holder
Journal: Antimicrob Agents Chemother Date: 2015-12-28 Impact factor: 5.191

8. SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.

Authors: Wenlin Huang; Kayode K Ojo; Zhongsheng Zhang; Kasey Rivas; Rama Subba Rao Vidadala; Suzanne Scheele; Amy E DeRocher; Ryan Choi; Matthew A Hulverson; Lynn K Barrett; Igor Bruzual; Latha Kallur Siddaramaiah; Keshia M Kerchner; Matthew D Kurnick; Gail M Freiberg; Dale Kempf; Wim G J Hol; Ethan A Merritt; Georg Neckermann; Eugenio L de Hostos; Nina Isoherranen; Dustin J Maly; Marilyn Parsons; J Stone Doggett; Wesley C Van Voorhis; Erkang Fan
Journal: ACS Med Chem Lett Date: 2015-10-22 Impact factor: 4.345

9. Calcium and a calcium-dependent protein kinase regulate gamete formation and mosquito transmission in a malaria parasite.

Authors: Oliver Billker; Sandrine Dechamps; Rita Tewari; Gerald Wenig; Blandine Franke-Fayard; Volker Brinkmann
Journal: Cell Date: 2004-05-14 Impact factor: 41.582

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

8 in total

1. Development of 5-Aminopyrazole-4-carboxamide-based Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.

Authors: Wenlin Huang; Matthew A Hulverson; Ryan Choi; Samuel L M Arnold; Zhongsheng Zhang; Molly C McCloskey; Grant R Whitman; Robert C Hackman; Kasey L Rivas; Lynn K Barrett; Kayode K Ojo; Wesley C Van Voorhis; Erkang Fan
Journal: J Med Chem Date: 2019-03-15 Impact factor: 7.446

2. 5-Aminopyrazole-4-Carboxamide-Based Compounds Prevent the Growth of Cryptosporidium parvum.

Authors: Wenlin Huang; Ryan Choi; Matthew A Hulverson; Zhongsheng Zhang; Molly C McCloskey; Deborah A Schaefer; Grant R Whitman; Lynn K Barrett; Rama Subba Rao Vidadala; Michael W Riggs; Dustin J Maly; Wesley C Van Voorhis; Kayode K Ojo; Erkang Fan
Journal: Antimicrob Agents Chemother Date: 2017-07-25 Impact factor: 5.191

3. 7 H-Pyrrolo[2,3- d]pyrimidin-4-amine-Based Inhibitors of Calcium-Dependent Protein Kinase 1 Have Distinct Inhibitory and Oral Pharmacokinetic Characteristics Compared with 1 H-Pyrazolo[3,4- d]pyrimidin-4-amine-Based Inhibitors.

Authors: Rama S R Vidadala; Martin Golkowski; Matthew A Hulverson; Ryan Choi; Molly C McCloskey; Grant R Whitman; Wenlin Huang; Samuel L M Arnold; Lynn K Barrett; Erkang Fan; Ethan A Merritt; Wesley C Van Voorhis; Kayode K Ojo; Dustin J Maly
Journal: ACS Infect Dis Date: 2018-03-16 Impact factor: 5.084

Review 4. Taming the Boys for Global Good: Contraceptive Strategy to Stop Malaria Transmission.

Authors: Ryan Choi; Samantha A Michaels; Emmanuel C Onu; Matthew A Hulverson; Aparajita Saha; Morenike E Coker; Janis C Weeks; Wesley C Van Voorhis; Kayode K Ojo
Journal: Molecules Date: 2020-06-16 Impact factor: 4.411

5. 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