Diamine derivatives with antiparasitic activities.
There are a lack of effective chemotherapies for many parasitic diseases. Polyamine pathways have been reported as potential targets for the development of new chemotherapies against parasitic diseases. In the present study, different libraries of substituted diamines totalling 78 compounds have been synthesized on solid support and their activities against malaria and leishmania parasites have been determined. Most active compounds demonstrated submicromolar activities against both organisms and their structure-activity relationships are discussed.
Labadie
Guillermo R
GR
Department of Medicinal Chemistry, School of Pharmacy, National Center of Natural Product Research, University of Mississippi, University, MS 38677, USA.
Choi
Seoung Ryoung
SR
Avery
Mitchell A
MA
D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D066298:In Vitro Techniques; D007893:Leishmania donovani / Q000187:drug effects*; D007990:Libraries; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000977:Antiparasitic Agents; D003959:Diamines