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  • team
  • department
  • center
  • program_project
  • nrc
  • whocc
  • project
  • software
  • tool
  • patent
  • Administrative Staff
  • Clinical Research Assistant
  • Graduate Student
  • Lab assistant
  • Non-permanent Researcher
  • Permanent Researcher
  • PhD Student
  • Physician
  • Post-doc
  • Project Manager
  • Research Engineer
  • Retired scientist
  • Technician
  • Undergraduate Student
  • Visiting Scientist
  • Deputy Director of Center
  • Deputy Director of Department
  • Deputy Director of National Reference Center
  • Director of Center
  • Director of Department
  • Director of Institute
  • Director of National Reference Center
  • Group Leader
  • Head of Facility
  • Head of Structure
  • Honorary President of the Departement
  • Labex Coordinator
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Starting Date
01
Oct 2014
Ending Date
30
Sep 2017
Status
Ongoing
Members
9
Structures
4

About

Concerted effort to address rational drug design against Chagas disease

Through a multidisciplinary approach that combine medicinal chemistry, structural bioinformatics, molecular docking and immunobiology of the infectious process, we identified two new inhibitors of an essential enzyme to T. cruzi, the parasite at the origin of Chagas infection and pathology. More than 60 analogues were then designed and synthesized by Medicinal Chemistry according to the most relevant molecular modeling data. Functional analysis ofsome of the new TcPRAC inhibitors showed that they exhibit low toxicity on green monkey kidney cells in culture, decrease in vitro cellular infection and parasite multiplication and fate in a dose-response manner. Continuing pharmacomodulations are in progress to optimize the biodisponibility and the trypanosomicide and/or trypanostatic effect of these new compounds. 

Rac

Fundings