Antileishmanial structure-activity relationships of synthetic phospholipids: in vitro and in vivo activities of selected derivatives.
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.
Seifert
Karin
K
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom. karin.seifert@lshtm.ac.uk
Lemke
Andreas
A
Croft
Simon L
SL
Kayser
Oliver
O
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006224:Cricetinae; D006801:Humans; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D007928:Lethal Dose 50; D015394:Molecular Structure; D010743:Phospholipids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D010743:Phospholipids