130402-63-0Relevant academic research and scientific papers
Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands
Szczepańska, Katarzyna,Karcz, Tadeusz,Siwek,Kuder, Kamil J.,Latacz, Gniewomir,Bednarski,Szafarz, Ma?gorzata,Hagenow, Stefanie,Lubelska, Annamaria,Olejarz-Maciej, Agnieszka,Sobolewski, Micha?,Mika,Kotańska, Magdalena,Stark, Holger,Kie?-Kononowicz, Katarzyna
supporting information, (2019/07/31)
A novel series of 4-pyridylpiperazine derivatives with varying alkyl linker length and eastern part substituents proved to be potent histamine H3 receptor (hH3R) ligands in the nanomolar concentration range. While paying attention to
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials
Jensen,Ager,Bliss,Canfield,Kotecka,Rieckmann,Terpinski,Jacobus
, p. 3925 - 3931 (2007/10/03)
A total of 34 analogues of the biguanide PS-15 (5s), a prodrug of the diaminotriazine WR-99210 (8s), have been prepared. Several of them, such as 5b (PS-33) and 5m (PS-26), maintain or exceed the in vivo activity of PS-15 while not requiring the use of highly regulated starting materials. The putative diaminotriazine metabolites of these new analogues (compounds 8) have also been prepared and shown to maintain the activity against resistant P. falciparum strains. The structure-activity relationships of biguanides 5 and putative metabolites 8 are discussed.
