《Design, diversity-oriented synthesis and biological evaluation of novel heterocycle derivatives as non-nucleoside HBV capsid protein inhibitors》 was written by Jia, Haiyong; Yu, Ji; Du, Xianhong; Cherukupalli, Srinivasulu; Zhan, Peng; Liu, Xinyong. SDS of cas: 4637-24-5 And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
This study focous on scaffold hopping, bioisosterism, and pharmacophore hybrid-based strategies to design and synthesize six series of various heterocycle derivatives (pyrazole, thiazole, pyrazine, pyrimidine, and pyridine) and screened for in vitro anti-HBV non-nucleoside activity. Drug candidate NZ-4 and AT-130 were used as lead compounds Several compounds exhibited prominent anti-HBV activity compared to lead compound NZ-4 and pos. drug Lamivudine, especially compound II-8b, showed the most prominent anti-HBV DNA replication activity (IC50 = 2.2 ± 1.1μM). Also compounds IV-8e and VII-5b showed the best in vitro anti-HBsAg secretion (IC50 = 3.8 ± 0.7μM, CC50 > 100μM) and anti-HBeAg secretion (IC50 = 9.7 ± 2.8μM, CC50 > 100μM) resp. Besides, II-8b was interact HBV capsid protein with good affinity constants (KD = 60.0μM), which was equivalent to lead compound NZ-4 (KD = 50.6μM). The preliminary structure-activity relationships (SARs) of the newly synthesized compounds were summarized, which may help researchers to discover more potent anti-HBV agents. The results came from multiple reactions, including the reaction of N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5SDS of cas: 4637-24-5)
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.SDS of cas: 4637-24-5
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem