1607830-85-2Relevant academic research and scientific papers
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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, (2014/06/11)
The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a Plasmodium parasite.
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
, 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.
