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Antimicrobial Agents and Chemotherapy, December 2007, p. 4525-4528, Vol. 51, No. 12
0066-4804/07/$08.00+0     doi:10.1128/AAC.00465-07
Copyright © 2007, American Society for Microbiology. All Rights Reserved.

Antileishmanial Structure-Activity Relationships of Synthetic Phospholipids: In Vitro and In Vivo Activities of Selected Derivatives{triangledown} ,{dagger}

Karin Seifert,1* Andreas Lemke,2 Simon L. Croft,1 and Oliver Kayser2

Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom,1 Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands2

Received 4 April 2007/ Returned for modification 26 June 2007/ Accepted 23 September 2007

Antileishmanial activities of 91 synthetic phospholipids against Leishmania donovani were evaluated in vitro and cytotoxicity assessed against two mammalian cell lines. Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity.

* Corresponding author. Mailing address: Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom. Phone: 44 (0)20 7927 2643. Fax: 44 (0)20 7637 4314. E-mail: karin.seifert{at}lshtm.ac.uk

{triangledown} Published ahead of print on 1 October 2007.

{dagger} Supplemental material for this article may be found at http://aac.asm.org/.

Antimicrobial Agents and Chemotherapy, December 2007, p. 4525-4528, Vol. 51, No. 12
0066-4804/07/$08.00+0     doi:10.1128/AAC.00465-07
Copyright © 2007, American Society for Microbiology. All Rights Reserved.





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