Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine

Authors
Chibale, K Haupt, H Kendrick, H Yardley, V Saravanamuthu, A Fairlamb, AH Croft, SL
Citation
K. Chibale et al., Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine, BIOORG MED, 11(19), 2001, pp. 2655-2657
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
19
Year of publication
2001
Pages
2655 - 2657
Database
ISI
SICI code
0960-894X(20011008)11:19<2655:AACEOS>2.0.ZU;2-Q
Abstract
Sulfonamide and urea derivatives of quinacrine with varying methylene space r lengths were synthesised and tested for inhibition of trypanothione reduc tase (TryR) and for activity in vitro against strains of the parasitic prot ozoa Trypanosoma, Leishmania, and Plasmodium. These derivatives are superio r inhibitors of TryR relative to quinacrine with the best compound being 40 times more potent. Urea derivatives generally displayed good in vitro acti vity against all parasites. (C) 2001 Elsevier Science Ltd. All rights reser ved.