TY - JOUR
T1 - Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine
AU - Chibale, Kelly
AU - Haupt, Hayley
AU - Kendrick, Howard
AU - Yardley, Vanessa
AU - Saravanamuthu, Ahilan
AU - Fairlamb, Alan H.
AU - Croft, Simon L.
N1 - Funding Information:
Financial support was through Grants 052075/Z/97 and 2039478 from the Wellcome Trust and National Research Foundation of South Africa respectively (KC), and UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases (HK, VY, SLC). AHF is supported by the Wellcome Trust.
PY - 2001/10/8
Y1 - 2001/10/8
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0035829161&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(01)00528-5
DO - 10.1016/S0960-894X(01)00528-5
M3 - Article
C2 - 11551771
AN - SCOPUS:0035829161
SN - 0960-894X
VL - 11
SP - 2655
EP - 2657
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 19
ER -