1062608-42-7Relevant articles and documents
Synthesis method of heterocyclic substituted coelenterazine compound
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Paragraph 0132-0133, (2021/10/27)
The invention provides a compound, which is a compound as shown in a formula (I), or a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound as shown in the formula (I). The compound and 2-aminopyrazine can be subjected to one-step cyclization under an acidic condition, and various R-2-position heterocyclic ring or heteroaromatic ring substituted coelenterazine derivatives can be rapidly generated.
NEW ANTI-MALARIAL AGENTS
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Page/Page column 19, (2017/02/09)
The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity
Younis, Yassir,Douelle, Frederic,González Cabrera, Diego,Le Manach, Claire,Nchinda, Aloysius T.,Paquet, Tanya,Street, Leslie J.,White, Karen L.,Zabiulla, K. Mohammed,Joseph, Jayan T.,Bashyam, Sridevi,Waterson, David,Witty, Michael J.,Wittlin, Sergio,Charman, Susan A.,Chibale, Kelly
supporting information, p. 8860 - 8871 (2013/12/04)
Replacement of the pyridine core of antimalarial 3,5-diaryl-2- aminopyridines led to the identification of a novel series of pyrazine analogues with potent oral antimalarial activity. However, other changes to the pyridine core and replacement or substitution of the 2-amino group led to loss of antimalarial activity. The 3,5-diaryl-2-aminopyrazine series showed impressive in vitro antiplasmodial activity against the K1 (multidrug resistant) and NF54 (sensitive) strains of Plasmodium falciparum in the nanomolar IC50 range of 6-94 nM while also demonstrating good in vitro metabolic stability in human liver microsomes. In the Plasmodium berghei mouse model, this series generally exhibited good efficacy at low oral doses. One of the frontrunner compounds, 4, displayed potent in vitro antiplasmodial activity with IC 50 values of 8.4 and 10 nM against the K1 and NF54 strains, respectively. When evaluated in P. berghei-infected mice, compound 4 was completely curative at an oral dose of 4 × 10 mg/kg.
ANTI -MALARIAL AGENTS
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Page/Page column 30, (2013/08/28)
The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.