TY - JOUR
T1 - Synthesis and biological evaluation of 2-substituted vinylgembisphosphonates against Plasmodium falciparum and Trypanosoma brucei
AU - Simelane, Siphamandla B.
AU - Ikhile, Monisola I.
AU - Ndinteh, Derek T.
AU - Mbianda, Xavier Y.
N1 - Publisher Copyright:
© 2020, © 2020 Taylor & Francis Group, LLC.
PY - 2020/7/2
Y1 - 2020/7/2
N2 - A 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.
AB - A 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.
KW - antimalarial activity
KW - antitrypasomal activity
KW - drug resistance
KW - Substituted vinyl gem-bisphosphonic acids
UR - http://www.scopus.com/inward/record.url?scp=85079758463&partnerID=8YFLogxK
U2 - 10.1080/10426507.2020.1728757
DO - 10.1080/10426507.2020.1728757
M3 - Article
AN - SCOPUS:85079758463
SN - 1042-6507
VL - 195
SP - 556
EP - 561
JO - Phosphorus, Sulfur and Silicon and the Related Elements
JF - Phosphorus, Sulfur and Silicon and the Related Elements
IS - 7
ER -
