1.
Bioorg Med Chem Lett
; 18(20): 5399-401, 2008 Oct 15.
Article
in English
| MEDLINE
| ID: mdl-18829314
ABSTRACT
Efficient synthetic routes have been developed for the preparation of two new polyazamacrocycles tagged with structural motifs recognised by the Trypanosoma brucei P2 aminopurine transporter. Biological testing of these compounds showed highly selective anti-protozoal activity against trypanosomes.
Subject(s)
Antiprotozoal Agents/pharmacology , Benzamidines/chemistry , Chemistry, Pharmaceutical/methods , Guanidine/chemistry , Trypanosomiasis, African/drug therapy , Trypanosomiasis, African/metabolism , Amino Acid Motifs , Animals , Biological Transport , Cell Line , Drug Design , Humans , Models, Chemical , Plasmodium falciparum/metabolism , Purines/chemistry
2.
Bioorg Med Chem Lett
; 18(7): 2455-8, 2008 Apr 01.
Article
in English
| MEDLINE
| ID: mdl-18313921
ABSTRACT
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.
