A novel microwave synthesis of quinoline-3-carboxylic acid derivatives for treatment against human African trypanosomiasis.
A series of quinoline-3-carboxylic acid derivatives has been synthesized with easy reaction conditions (in aqueous micellar microreactors and using microwave irradiation) and tested for its biological activity against human African trypanosomiasis (HAT). From this series, several derivatives of quinoline-3-carboxylic acid such as 23 and 24 exhibited potent activity against Trypanosoma brucei in vitro and had low cytotoxicity. The combination of electron withdrawing and donating groups in the structure seems to be the crucial factor to inhibit T. brucei.
Natural Product and Medicinal Chemistry Research Group, Division of Pharmaceutical chemistry, Rhodes University, Grahamstown 6140, South Africa. b.samant@ru.ac.za
Bhupesh S
BS
Samant
Nyaradzai
N
Nyangari
D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D051379:Mice; D008872:Microwaves; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy / Q000469:parasitology
D011804:Quinolines; D014344:Trypanocidal Agents