Rasina, Dace; Stakanovs, Georgijs; Kanepe-Lapsa, Iveta; Bobrovs, Raitis; Jaudzems, Kristaps; Jirgensons, Aigars published the artcile< Synthesis of 2-aminopyridopyrimidinones and their plasmepsin I, II, IV inhibition potency>, Reference of 870997-85-6, the main research area is aminopyridopyrimidinone preparation antimalarial SAR.
2-Aminoquinazolin-4(3H)-one-based inhibitors, 2-aminopyrido[2,3-d]-, -[3,2-d]-, and -[4,3-d]pyrimidin-4(3H)-ones beared subpocket-specific substituents at position 7 were prepared and tested for their Plm I, II, IV inhibition potency. The position of the nitrogen atom in 2-aminopyridopyrimidinones played significant role in the inhibitory potency against Plms. Pyrido[2,3-d]pyrimidin-4(3H)-one derivatives showed poor inhibitory potency against Plms I, II, IV irresp. of the substituent at position 7. However, pyrido[4,3-d]pyrimidin-4(3H)-ones and pyrido[3,2-d]pyrimidin-4(3H)-ones were more appropriate scaffolds for Plm inhibitor development. Particularly, 2-amino-7-[4-(3-phenylpropyl)phenyl]-3-[(tetrahydrofuran-2-yl)methyl]pyrido[3,2-d]pyrimidin-4(3H)-one showed very high potency against Plm IV subtype and high selectivity against human aspartic protease, cathepsin D.
Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about Antimalarials. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Reference of 870997-85-6.