1224624-75-2Relevant articles and documents
Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase1
Spinks, Daniel,Ong, Han B.,Mpamhanga, Chidochangu P.,Shanks, Emma J.,Robinson, David A.,Collie, Iain T.,Read, Kevin D.,Frearson, Julie A.,Wyatt, Paul G.,Brenk, Ruth,Fairlamb, Alan H.,Gilbert, Ian H.
, p. 302 - 308 (2012/01/12)
Genetic studies indicate that the enzyme pteridine reductase1 (PTR1) is essential for the survival of the protozoan parasite Trypanosoma brucei. Herein, we describe the development and optimisation of a novel series of PTR1 inhibitors, based on benzo[d]im
One scaffold, three binding modes: Novel and selective pteridine reductase 1 inhibitors derived from fragment hits discovered by virtual screening
Mpamhanga, Chidochangu P.,Spinks, Daniel,Tulloch, Lindsay B.,Shanks, Emma J.,Robinson, David A.,Collie, Iain T.,Fairlamb, Alan H.,Wyatt, Paul G.,Frearson, Julie A.,Hunter, William N.,Gilbert, Ian H.,Brenk, Ruth
experimental part, p. 4454 - 4465 (2010/03/01)
The enzyme pteridine reductase 1 (PTR1) is a potential target for new compounds to treat human African trypanosomiasis. A virtual screening campaign for fragments inhibiting PTR1 was carried out. Two novel chemical series were identified containing aminob
