Synthesis and anti-protozoal activity of C2-substituted polyazamacrocycles.
A focused library of C2-substituted-1,4,7,10-tetraazacyclododecanes was synthesised and the compounds were tested for their ability to kill trypanosome and malaria parasites. Several compounds showed significant in vitro activity and were selectively active against the parasites over human embryonic kidney cells used as a counter screen.
Reid
Caroline M
CM
WestCHEM, Department of Chemistry, The Joseph Black Building, University of Glasgow, Glasgow G12 8QQ, UK.
Ebikeme
Charles
C
Barrett
Michael P
MP
Patzewitz
Eva-Maria
EM
Müller
Sylke
S
Robins
David J
DJ
Sutherland
Andrew
A
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D001372:Aza Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007668:Kidney / Q000166:cytology / Q000187:drug effects* / Q000196:embryology; D047028:Macrocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D008288:Malaria / Q000188:drug therapy* / Q000469:parasitology; D008956:Models, Chemical; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014345:Trypanosoma / Q000187:drug effects*
D000981:Antiprotozoal Agents; D001372:Aza Compounds; D047028:Macrocyclic Compounds