Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine.

K Chibale; H Haupt; H Kendrick; V Yardley; A Saravanamuthu; AH Fairlamb; SL Croft ORCID logo; (2001) Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine. Bioorganic & medicinal chemistry letters, 11 (19). pp. 2655-2657. ISSN 0960-894X DOI: 10.1016/s0960-894x(01)00528-5
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Sulfonamide and urea derivatives of quinacrine with varying methylene spacer lengths were synthesised and tested for inhibition of trypanothione reductase (TryR) and for activity in vitro against strains of the parasitic protozoa Trypanosoma, Leishmania, and Plasmodium. These derivatives are superior inhibitors of TryR relative to quinacrine with the best compound being 40 times more potent. Urea derivatives generally displayed good in vitro activity against all parasites.
Item Type Article
Keywords Trypanothione reductase inhibitors, trypanosoma-cruzi, invitro, antimalarial, Animal, Antiprotozoal Agents, chemical synthesis, chemistry, pharmacology, Leishmania, drug effects, Parasitic Sensitivity Tests, Plasmodium, drug effects, Quinacrine, analogs & derivatives, chemical synthesis, chemistry, pharmacology, Sulfonamides, chemistry, Support, Non-U.S. Gov't, Trypanosoma, drug effects, Urea, chemistry
ISI 171174300022

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