Jakubkiene, Virginija; Valiulis, Gabrielius Ernis; Schweipert, Markus; Zubriene, Asta; Matulis, Daumantas; Meyer-Almes, Franz-Josef; Tumkevicius, Sigitas published an article in 2022, the title of the article was Synthesis and HDAC inhibitory activity of pyrimidine-based hydroxamic acids.COA of Formula: C5H6N2O2 And the article contains the following content:
Here, the synthesis of new compounds in which a hydroxamic acid residue was attached to differently substituted pyrimidine rings via a methylene group bridge of varying length as potential HDAC inhibitors was described. The target compounds were obtained by alkylation of 2-(alkylthio)pyrimidin-4(3H)-ones with Et 2-bromoethanoate, Et 4-bromobutanoate, or Me 6-bromohexanoate followed by aminolysis of the obtained esters with hydroxylamine. Oxidation of the 2-methylthio group to the methylsulfonyl group and following treatment with amines resulted in the formation of the corresponding 2-amino-substituted derivatives, the ester group of which reacted with hydroxylamine to give the corresponding hydroxamic acids. The synthesized hydroxamic acids were tested as inhibitors of the HDAC4 and HDAC8 isoforms. Among the synthesized pyrimidine-based hydroxamic acids -hydroxy-6-[6-methyl-2-(methylthio)-5-propylpyrimidin-4-yloxy]hexanamide was found to be the most potent inhibitor of both the HDAC4 and HDAC8 isoforms, with an IC50 of 16.6μM and 1.2μM, resp. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).COA of Formula: C5H6N2O2
The Article related to pyrimidine based hydroxamic acid preparation hdac inhibitor, hdac inhibitors, alkylation, aminolysis, hydroxamic acid, pyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C5H6N2O2
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia