1.
Bioorg Med Chem Lett
; 18(20): 5399-401, 2008 Oct 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18829314
RESUMEN
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.
Asunto(s)
Antiprotozoarios/farmacología , Benzamidinas/química , Química Farmacéutica/métodos , Guanidina/química , Tripanosomiasis Africana/tratamiento farmacológico , Tripanosomiasis Africana/metabolismo , Secuencias de Aminoácidos , Animales , Transporte Biológico , Línea Celular , Diseño de Fármacos , Humanos , Modelos Químicos , Plasmodium falciparum/metabolismo , Purinas/química
2.
Bioorg Med Chem Lett
; 18(7): 2455-8, 2008 Apr 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18313921
RESUMEN
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.