Related Products of 519032-07-6On November 21, 2018 ,《Discovery and Structure-Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-D-ribose 2′-Oxidase》 appeared in Journal of Medicinal Chemistry. The author of the article were Oh, Sangmi; Park, Yumi; Engelhart, Curtis A.; Wallach, Joshua B.; Schnappinger, Dirk; Arora, Kriti; Manikkam, Michelle; Gac, Brian; Wang, Hongwu; Murgolo, Nicholas; Olsen, David B.; Goodwin, Michael; Sutphin, Michelle; Weiner, Danielle M.; Via, Laura E.; Boshoff, Helena I. M.; Barry, Clifton E.. The article conveys some information:
Magnesium plays an important role in infection with Mycobacterium tuberculosis (Mtb) as a signal of the extracellular environment, as a cofactor for many enzymes, and as a structural element in important macromols. Raltegravir, an antiretroviral drug that inhibits HIV-1 integrase is known to derive its potency from selective sequestration of active-site magnesium ions in addition to binding to a hydrophobic pocket. In order to determine if essential Mtb-related phosphoryl transfers could be disrupted in a similar manner, a directed screen of known mols. with integrase inhibitor-like pharmacophores (N-alkyl-5-hydroxypyrimidinone carboxamides) was performed. Initial hits afforded compounds with low-micromolar potency against Mtb, acceptable cytotoxicity and PK characteristics, and robust SAR. Elucidation of the target of these compounds revealed that they lacked magnesium dependence and instead disappointingly inhibited a known promiscuous target in Mtb, decaprenylphosphoryl-β-D-ribose 2′-oxidase (DprE1, Rv3790).Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6Related Products of 519032-07-6) was used in this study.
Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Related Products of 519032-07-6
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia