1402173-92-5Relevant academic research and scientific papers
Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues
Large, Jonathan M.,Osborne, Simon A.,Smiljanic-Hurley, Ela,Ansell, Keith H.,Jones, Hayley M.,Taylor, Debra L.,Clough, Barbara,Green, Judith L.,Holder, Anthony A.
, p. 6019 - 6024 (2013/10/22)
The structural diversity and SAR in a series of imidazopyridazine inhibitors of Plasmodium falciparum calcium dependent protein kinase 1 (PfCDPK1) has been explored and extended. The opportunity to further improve key ADME parameters by means of lowering log D was identified, and this was achieved by replacement of a six-membered (hetero)aromatic linker with a pyrazole. A short SAR study has delivered key examples with useful in vitro activity and ADME profiles, good selectivity against a human kinase panel and improved levels of lipophilic ligand efficiency. These new analogues thus provide a credible additional route to further development of the series.
