Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine

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 - https://www.scopus.com/pages/publications/0035829161

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 -