On February 25, 2018, Tuo, Wei; Bollier, Melanie; Leleu-Chavain, Natascha; Lemaire, Lucas; Barczyk, Amelie; Dezitter, Xavier; Klupsch, Frederique; Szczepanski, Fabien; Spencer, John; Chavatte, Philippe; Millet, Regis published an article.Electric Literature of 5098-14-6 The title of the article was Development of novel oxazolo[5,4-d]pyrimidines as competitive CB2 neutral antagonists based on scaffold hopping. And the article contained the following:
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. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Electric Literature of 5098-14-6
The Article related to oxazolopyrimidine preparation cytotoxicity sar cannabinoid receptor antagonist, cb(2) receptor, cannabinoid, neutral antagonist, oxazolo[5,4-d]pyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 5098-14-6
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts