title: Synthesis of novel benzamidine- and guanidine-derived polyazamacrocycles: Selective anti-protozoal activity for human African trypanosomiasis.
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.
authors.affiliation: WestCHEM, Department of Chemistry, The Joseph Black Building, University of Glasgow, Glasgow G12 8QQ, UK.
authors.forename: Caroline M
authors.initials: CM
authors.lastname: Reid
authors.forename: Charles
authors.initials: C
authors.lastname: Ebikeme
authors.forename: Michael P
authors.initials: MP
authors.lastname: Barrett
authors.forename: Eva-Maria
authors.initials: EM
authors.lastname: Patzewitz
authors.forename: Sylke
authors.initials: S
authors.lastname: Müller
authors.forename: David J
authors.initials: DJ
authors.lastname: Robins
authors.forename: Andrew
authors.initials: A
authors.lastname: Sutherland
mesh_terms: 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*
chemical_list: D000981:Antiprotozoal Agents; D001550:Benzamidines; D011687:Purines; D019791:Guanidine; C032157:benzamidine