886361-98-4Relevant academic research and scientific papers
Lead optimization of imidazopyrazines: A new class of antimalarial with activity on Plasmodium liver stages
Zou, Bin,Nagle, Advait,Chatterjee, Arnab K.,Leong, Seh Yong,Tan, Liying Jocelyn,Sim, Wei Lin Sandra,Mishra, Pranab,Guntapalli, Prasuna,Tully, David C.,Lakshminarayana, Suresh B.,Lim, Chek Shik,Tan, Yong Cheng,Abas, Siti Nurdiana,Bodenreider, Christophe,Kuhen, Kelli L.,Gagaring, Kerstin,Borboa, Rachel,Chang, Jonathan,Li, Chun,Hollenbeck, Thomas,Tuntland, Tove,Zeeman, Anne-Marie,Kocken, Clemens H. M.,McNamara, Case,Kato, Nobutaka,Winzeler, Elizabeth A.,Yeung, Bryan K. S.,Diagana, Thierry T.,Smith, Paul W.,Roland, Jason
supporting information, p. 947 - 950 (2014/10/15)
Imidazopyridine 1 was identified from a phenotypic screen against P. falciparum (Pf) blood stages and subsequently optimized for activity on liver-stage schizonts of the rodent parasite P. yoelii (Py) as well as hypnozoites of the simian parasite P. cynomolgi (Pc). We applied these various assays to the cell-based lead optimization of the imidazopyrazines, exemplified by 3 (KAI407), and show that optimized compounds within the series with improved pharmacokinetic properties achieve causal prophylactic activity in vivo and may have the potential to target the dormant stages of P. vivax malaria.
ORGANIC COMPOUNDS
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Page/Page column 122, (2009/05/28)
Compounds of formula (I): in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treati ng diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical composit ions that contain the compounds and processes for preparing the compounds are also described.
