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Synthesis and Activity of a New Series of Antileishmanial Agents.
Kanwar, Ankush; Eduful, Benjamin J; Barbeto, Linda; Carletti Bonomo, Piero; Lemus, Andrea; Vesely, Brian A; Mutka, Tina S; Azhari, Ala; Kyle, Dennis E; Leahy, James W.
Afiliación
  • Kanwar A; Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
  • Eduful BJ; Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
  • Barbeto L; Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
  • Carletti Bonomo P; Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
  • Lemus A; Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
  • Vesely BA; Department of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Suite 304, Tampa, Florida 33612, United States.
  • Mutka TS; Department of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Suite 304, Tampa, Florida 33612, United States.
  • Azhari A; Department of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Suite 304, Tampa, Florida 33612, United States.
  • Kyle DE; Department of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Suite 304, Tampa, Florida 33612, United States.
  • Leahy JW; Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
ACS Med Chem Lett ; 8(8): 797-801, 2017 Aug 10.
Article en En | MEDLINE | ID: mdl-28835791
ABSTRACT
We have determined that tetrahydroindazoles such as 1 show potent activity against Leishmania donovani, the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of 1 have previously been explored, we present here our efforts to optimize their activity against L. donovani via the synthesis of novel analogues designed to probe the hydrophobic pocket of the protozoan Hsp90 orthologue, specifically through the auspices of functionalization of an amine embedded into the scaffold.
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Texto completo: 1 Bases de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos

Texto completo: 1 Bases de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos