Synthesis and antitrypanosomal activities of novel pyridylchalcones
Date
2017-01-23
Advisors
Journal Title
Journal ISSN
ISSN
0223-5234
Volume Title
Publisher
Elsevier
Type
Article
Peer reviewed
Yes
Abstract
A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC50 value of 0.29 M. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT).
Description
Collaboration with the London School of Hygiene and Tropical Medicine.
The file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.
Keywords
Neglected tropical disease, Trypanosoma brucei, Leishmania donovani, Pyridylchalcone, Claisen-Schmidt
Citation
Bhambra, A.S et al. (2017) Synthesis and antitrypanosomal activities of novel pyridylchalcones. European Journal of Medicinal Chemistry, 128, pp. 213-218
Rights
Research Institute
Institute for Allied Health Sciences Research
Leicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)
Leicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)