Tuo, Wei published the artcileDevelopment of novel oxazolo[5,4-d]pyrimidines as competitive CB2 neutral antagonists based on scaffold hopping, Application In Synthesis of 5098-14-6, the publication is European Journal of Medicinal Chemistry (2018), 68-78, database is CAplus and MEDLINE.
A series of novel oxazolo[5,4-d]pyrimidines I [R1 = H, Cl, F, CF3; R2 = H, Me; R3 = n-Bu, cyclohexylmethyl, 1-methylpiperazinyl, etc.] was designed via a scaffold hopping strategy and synthesized through a newly developed approach. All these compounds I were evaluated for their biol. activity toward CB1/CB2 cannabinoid receptors, their metabolic stability in mice liver microsomes and their cytotoxicity against several cell lines. Eight compounds I [R1 = Cl, CF3; R2 = H, Me; R3 = 1-methylpiperazinyl, 1-ethylpiperazinyl, 1-acetylpiperazinyl] were identified as CB2 ligands with Ki values less than 1 ΜM. It was noteworthy that compounds I [R1 = Cl; R2 = Me; R3 = 1-methylpiperazinyl, 1-ethylpiperazinyl] showed CB2 binding affinity in the nanomolar range and significant selectivity over CB1 receptors. Interestingly, functionality studies imply that they behaved as competitive neutral antagonists. Moreover, all tested compounds I were devoid of cytotoxicity toward several cell lines, including Chinese hamster ovary cells (CHO) and human colorectal adenocarcinoma cells HT29.
European Journal of Medicinal Chemistry published new progress about 5098-14-6. 5098-14-6 belongs to nitriles-buliding-blocks, auxiliary class Nitrile,Salt,Sulfonic acid,Amine,Benzene, name is 2-Aminomalononitrile 4-methylbenzenesulfonate, and the molecular formula is C12H16O3, Application In Synthesis of 5098-14-6.
Referemce:
https://en.wikipedia.org/wiki/Nitrile,
Nitriles – Chemistry LibreTexts