Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine


Chibale, K; Haupt, H; Kendrick, H; Yardley, V; Saravanamuthu, A; Fairlamb, AH; Croft, SL; (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: https://doi.org/10.1016/S0960-894X(01)00528-5

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Abstract

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. (C) 2001 Elsevier Science Ltd. All rights reserved.

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
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Leishmaniasis Group
PubMed ID: 11551771
Web of Science ID: 171174300022
URI: http://researchonline.lshtm.ac.uk/id/eprint/16569

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