SciELO - Scientific Electronic Library Online

vol.71Highly Sensitive Electrochemical Sensing Platform for the Detection of L-dopa Based on Electropolymerizing Glutathione Disulfide and Multi-walled Carbon Nanotube-modified Electrodes índice de autoresíndice de assuntospesquisa de artigos
Home Pagelista alfabética de periódicos  

Serviços Personalizados



Links relacionados

  • Em processo de indexaçãoCitado por Google
  • Em processo de indexaçãoSimilares em Google


South African Journal of Chemistry

versão On-line ISSN 1996-840X
versão impressa ISSN 0379-4350


BETECK, Richard M.; ISAACS, Michelle; HOPPE, Heinrich C.  e  KHANYE, Setshaba D.. Synthesis, in vitro Cytotoxicity and Trypanocidal Evaluation of Novel 1,3,6-Substituted Non-fluoroquinolones. S.Afr.j.chem. (Online) [online]. 2018, vol.71, pp.188-195. ISSN 1996-840X.

Sleeping sickness (trypanosomiasis) is a neglected tropical disease that affects mostly the poorest communities in sub-Saharan Africa. Toxic side effects associated with the use of current anti-trypanosomal drugs, which in some cases kill faster than the disease itself, necessitate the search for new drugs with better safety margins. To this effect, a small library bearing different substituents at position -1, -3, and -6 of the quinolone nucleus were synthesized and evaluated in vitro against HeLa cell lines and Trypanosoma brucei brucei for cytotoxicity and trypanocidal potentials, respectively. While most of these compounds showed no cytotoxic effect, they exhibited moderate to weak anti-trypanosomal activities. The SAR studies of this series provide new information worth considering in future exploration of the quinolone scaffold in search of more potent and safe trypanocidal agents.

Palavras-chave : Sleeping sickness; trypanosomiasis; quinolones; non-fluoroquinolones.

        · texto em Inglês     · Inglês ( pdf )


Creative Commons License Todo o conteúdo deste periódico, exceto onde está identificado, está licenciado sob uma Licença Creative Commons