Synthesis and biological evaluation of 2-substituted vinylgembisphosphonates against Plasmodium falciparum and Trypanosoma brucei |
| |
Authors: | Siphamandla B Simelane Monisola I Ikhile Xavier Y Mbianda |
| |
Institution: | Department of Applied Chemistry, University of Johannesburg, Doornfontein, South Africa |
| |
Abstract: | AbstractA series of 2-substituted vinylidene-1,1-bisphosphonate esters and their acids were synthesized and tested in vitro for activity against Plasmodium falciparum and Trypanosoma brucei. For each compound, % parasite viability in treated wells was calculated relative to untreated controls for both P. falciparum and T. brucei. Fifty percentage inhibitory concentration (IC50) was also determined for the compounds. Chloroquine and pentamidine were used as positive control drug standards for activity against P. falciparum and T. brucei, respectively. The esters had better antiparasitic activity compared to their corresponding acids. Some of the compounds reduced % parasite viability to as low as 24.3% for P. falciparum and down to 0.602% for T. brucei. Tetraethyl-2-(o-tolyl)-ethene-1,1-bisphosphonate (3b) recorded the best IC50 against T. brucei which was 0.0345?µmol/mL. |
| |
Keywords: | Substituted vinyl gem-bisphosphonic acids antimalarial activity antitrypasomal activity drug resistance |
|
|