Literature DB >> 28533246

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

Wenlin Huang1, Ryan Choi2, Matthew A Hulverson2, Zhongsheng Zhang1, Molly C McCloskey2, Deborah A Schaefer3, Grant R Whitman2, Lynn K Barrett2, Rama Subba Rao Vidadala4, Michael W Riggs3, Dustin J Maly1,4, Wesley C Van Voorhis2, Kayode K Ojo5, Erkang Fan6.   

Abstract

Cryptosporidium parvum calcium-dependent protein kinase 1 (CpCDPK1) is a promising target for drug development against cryptosporidiosis. We report a series of low-nanomolar CpCDPK1 5-aminopyrazole-4-carboxamide (AC) scaffold inhibitors that also potently inhibit C. parvum growth in vitro Correlation between anti-CpCDPK1 and C. parvum growth inhibition, as previously reported for pyrazolopyrimidines, was not apparent. Nonetheless, lead AC compounds exhibited a substantial reduction of parasite burden in the neonatal mouse cryptosporidiosis model when dosed at 25 mg/kg.
Copyright © 2017 American Society for Microbiology.

Entities:  

Keywords:  5-aminopyrazole-4-carboxamide; Cryptosporidium parvum; bumped kinase inhibitors

Mesh：

Substances：

Year:  2017        PMID： 28533246      PMCID： PMC5527629          DOI： 10.1128/AAC.00020-17

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  14 in total

Review 1.  A review of the global burden, novel diagnostics, therapeutics, and vaccine targets for cryptosporidium.

Authors:  William Checkley; A Clinton White; Devan Jaganath; Michael J Arrowood; Rachel M Chalmers; Xian-Ming Chen; Ronald Fayer; Jeffrey K Griffiths; Richard L Guerrant; Lizbeth Hedstrom; Christopher D Huston; Karen L Kotloff; Gagandeep Kang; Jan R Mead; Mark Miller; William A Petri; Jeffrey W Priest; David S Roos; Boris Striepen; R C Andrew Thompson; Honorine D Ward; Wesley A Van Voorhis; Lihua Xiao; Guan Zhu; Eric R Houpt
Journal:  Lancet Infect Dis       Date:  2014-09-29       Impact factor: 25.071

2.  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

3.  Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.

Authors:  Matthew A Hulverson; Sumiti Vinayak; Ryan Choi; Deborah A Schaefer; Alejandro Castellanos-Gonzalez; Rama S R Vidadala; Carrie F Brooks; Gillian T Herbert; Dana P Betzer; Grant R Whitman; Hayley N Sparks; Samuel L M Arnold; Kasey L Rivas; Lynn K Barrett; A Clinton White; Dustin J Maly; Michael W Riggs; Boris Striepen; Wesley C Van Voorhis; Kayode K Ojo
Journal:  J Infect Dis       Date:  2017-04-15       Impact factor: 5.226

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

Authors:  Wenlin Huang; Matthew A Hulverson; Zhongsheng Zhang; Ryan Choi; Kevin J Hart; Mark Kennedy; Rama Subba Rao Vidadala; Dustin J Maly; Wesley C Van Voorhis; Scott E Lindner; Erkang Fan; Kayode K Ojo
Journal:  Bioorg Med Chem Lett       Date:  2016-10-10       Impact factor: 2.823

5.  Apical organelle discharge by Cryptosporidium parvum is temperature, cytoskeleton, and intracellular calcium dependent and required for host cell invasion.

Authors:  Xian-Ming Chen; Steven P O'Hara; Bing Q Huang; Jeremy B Nelson; Jim Jung-Ching Lin; Guan Zhu; Honorine D Ward; Nicholas F LaRusso
Journal:  Infect Immun       Date:  2004-12       Impact factor: 3.441

6.  The infectivity of Cryptosporidium parvum in healthy volunteers.

Authors:  H L DuPont; C L Chappell; C R Sterling; P C Okhuysen; J B Rose; W Jakubowski
Journal:  N Engl J Med       Date:  1995-03-30       Impact factor: 91.245

Review 7.  Burden of disease from cryptosporidiosis.

Authors:  Debbie-Ann T Shirley; Shannon N Moonah; Karen L Kotloff
Journal:  Curr Opin Infect Dis       Date:  2012-10       Impact factor: 4.915

8.  Burden and aetiology of diarrhoeal disease in infants and young children in developing countries (the Global Enteric Multicenter Study, GEMS): a prospective, case-control study.

Authors:  Karen L Kotloff; James P Nataro; William C Blackwelder; Dilruba Nasrin; Tamer H Farag; Sandra Panchalingam; Yukun Wu; Samba O Sow; Dipika Sur; Robert F Breiman; Abu Sg Faruque; Anita Km Zaidi; Debasish Saha; Pedro L Alonso; Boubou Tamboura; Doh Sanogo; Uma Onwuchekwa; Byomkesh Manna; Thandavarayan Ramamurthy; Suman Kanungo; John B Ochieng; Richard Omore; Joseph O Oundo; Anowar Hossain; Sumon K Das; Shahnawaz Ahmed; Shahida Qureshi; Farheen Quadri; Richard A Adegbola; Martin Antonio; M Jahangir Hossain; Adebayo Akinsola; Inacio Mandomando; Tacilta Nhampossa; Sozinho Acácio; Kousick Biswas; Ciara E O'Reilly; Eric D Mintz; Lynette Y Berkeley; Khitam Muhsen; Halvor Sommerfelt; Roy M Robins-Browne; Myron M Levine
Journal:  Lancet       Date:  2013-05-14       Impact factor: 79.321

9.  A novel calcium-dependent protein kinase inhibitor as a lead compound for treating cryptosporidiosis.

Authors:  Alejandro Castellanos-Gonzalez; A Clinton White; Kayode K Ojo; Rama S R Vidadala; Zhongsheng Zhang; Molly C Reid; Anna M W Fox; Katelyn R Keyloun; Kasey Rivas; Ayesha Irani; Sara M Dann; Erkang Fan; Dustin J Maly; Wesley C Van Voorhis
Journal:  J Infect Dis       Date:  2013-07-21       Impact factor: 5.226

10.  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
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  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.  Pharmacokinetics and In Vivo Efficacy of Pyrazolopyrimidine, Pyrrolopyrimidine, and 5-Aminopyrazole-4-Carboxamide Bumped Kinase Inhibitors against Toxoplasmosis.

Authors:  Matthew A Hulverson; Igor Bruzual; Erin V McConnell; Wenlin Huang; Rama S R Vidadala; Ryan Choi; Samuel L M Arnold; Grant R Whitman; Molly C McCloskey; Lynn K Barrett; Kasey L Rivas; Suzanne Scheele; Amy E DeRocher; Marilyn Parsons; Kayode K Ojo; Dustin J Maly; Erkang Fan; Wesley C Van Voorhis; J Stone Doggett
Journal:  J Infect Dis       Date:  2019-04-16       Impact factor: 5.226

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

4.  Pyrrolopyrimidine Bumped Kinase Inhibitors for the Treatment of Cryptosporidiosis.

Authors:  Matthew A Hulverson; Ryan Choi; Rama S R Vidadala; Grant R Whitman; Venkata Narayana Vidadala; Kayode K Ojo; Lynn K Barrett; James J Lynch; Kennan Marsh; Dale J Kempf; Dustin J Maly; Wesley C Van Voorhis
Journal:  ACS Infect Dis       Date:  2021-02-10       Impact factor: 5.084

Review 5.  One health therapeutics: Target-Based drug development for cryptosporidiosis and other apicomplexa diseases.

Authors:  Wesley C Van Voorhis; Matthew A Hulverson; Ryan Choi; Wenlin Huang; Samuel L M Arnold; Deborah A Schaefer; Dana P Betzer; Rama S R Vidadala; Sangun Lee; Grant R Whitman; Lynn K Barrett; Dustin J Maly; Michael W Riggs; Erkang Fan; Thomas J Kennedy; Saul Tzipori; J Stone Doggett; Pablo Winzer; Nicoleta Anghel; Dennis Imhof; Joachim Müller; Andrew Hemphill; Ignacio Ferre; Roberto Sanchez-Sanchez; Luis Miguel Ortega-Mora; Kayode K Ojo
Journal:  Vet Parasitol       Date:  2020-12-15       Impact factor: 2.738

6.  Characterization of Calcium-Dependent Protein Kinases 3, a Protein Involved in Growth of Cryptosporidium parvum.

Authors:  Qiang Zhang; Yaqiong Guo; Na Li; Yu Li; Jiayuan Su; Rui Xu; Ziding Zhang; Yaoyu Feng; Lihua Xiao
Journal:  Front Microbiol       Date:  2020-05-08       Impact factor: 5.640

7.  Comparative Characterization of CpCDPK1 and CpCDPK9, Two Potential Drug Targets Against Cryptosporidiosis.

Authors:  Jiayuan Su; Yiting Shen; Na Li; Yu Li; Ziding Zhang; Lihua Xiao; Yaqiong Guo; Yaoyu Feng
Journal:  Microorganisms       Date:  2022-02-01

Review 8.  An update on Cryptosporidium biology and therapeutic avenues.

Authors:  Ajit Kumar Dhal; Chinmaya Panda; Soon-Il Yun; Rajani Kanta Mahapatra
Journal:  J Parasit Dis       Date:  2022-06-22
  8 in total

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