QUINOXALINE-BASED INHIBITORS OF MALARIAL PROTEASE PfSUB1

Authors

  • S. S. Kher Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia
  • M. Penzo Division of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K.
  • S. Fulle BioMed X Innovation Center, Im Neuenheimer Feld 583, 69120 Heidelberg, Germany
  • J. P. Ebejer InhibOx Ltd., Oxford Centre for Innovation, New Road, Oxford OX1 1BY, U.K.
  • P. W. Finn InhibOx Ltd., Oxford Centre for Innovation, New Road, Oxford OX1 1BY, U.K.
  • M. J. Blackman Division of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K.
  • A. Jirgensons Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia

DOI:

https://doi.org/10.1007/1779

Keywords:

quinoxaline, inhibitors, malaria, Malaria Box, PfSUB1 protease

Abstract

2,3-Bis(phenylamino)quinoxalines have been identified as a novel class of malarial protease PfSUB1 inhibitors by screening of Malaria Box compounds. The synthesis of analogs series and investigation of their inhibitory activity provided preliminary structure–activity relationship to create in silico models for binding of these compounds into the active site of PfSUB1.

How to Cite
Kher, S. S.; Penzo, M.; Fulle, S.; Ebejer, J. P.; Finn, P. W.; Blackman, M. J.; Jirgensons, A. Chem. Heterocycl. Compd. 2015, 50, 1457. [Khim. Geterotsikl. Soedin. 2014, 1583.]

For this article in the English edition see DOI 10.1007/s10593-014-1610-4

Author Biography

A. Jirgensons, Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia

Aigars Jirgensons

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Published

2014-10-13

Issue

No. 10 (2014)

Section

Original Papers