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Journal of Antimicrobial Chemotherapy (1992) 30, 827-832
© 1992 The British Society for Antimicrobial Chemotherapy

research-article

The activity of hydroxynaphthoquinones against Leishmania donovani

S. L. Croft*, J Hogg, W. E. Gutteridge, A. T. Hudson and A. W. Randall

Wellcome Research Laboratories Beckenham, Kent, BR3 3BS, UK

Received 18 March 1992; returned 28 July 1992; accepted 28 July 1992

The hydroxynaphthoquinoncs, buparvaquone, 250C80 and 56W82, showed high activity in vitro against Leishmania donovani amastigotes in mouse peritoneal macro phages, with ED50 values of 0-05, 2·95 and 13·82 µM, respectively. Fourteen other hydroxynaphthoquinones were tested, of which only 566C80 and 608C86 showed significant activity against amastigotes. Buparvaquone, 250C80 and 56W82 were also highly-active against cultured promastigotes. In a BALB/c mouse model, treatment with 100 mg/kg/day for five days with buparvaquone, 250C80 and 566C80 (atovaquone) reduced liver amastigote numbers by 60%, 22% and 30·5%, respectively.


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