Synthesis of novel benzamidine- and guanidine-derived polyazamacrocycles: Selective anti-protozoal activity for human African trypanosomiasis.
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.
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
D020816:Amino Acid Motifs; D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D001550:Benzamidines / Q000737:chemistry*; D001692:Biological Transport; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D019791:Guanidine / Q000737:chemistry*; D006801:Humans; D008956:Models, Chemical; D010963:Plasmodium falciparum / Q000378:metabolism; D011687:Purines / Q000737:chemistry; D014353:Trypanosomiasis, African / Q000188:drug therapy* / Q000378:metabolism*
D000981:Antiprotozoal Agents; D001550:Benzamidines; D011687:Purines; D019791:Guanidine; C032157:benzamidine