2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies was written by Yan, Gang;Hao, Lina;Niu, Yan;Huang, Wenjie;Wang, Wei;Xu, Fengrong;Liang, Lei;Wang, Chao;Jin, Hongwei;Xu, Ping. And the article was included in European Journal of Medicinal Chemistry in 2017.SDS of cas: 105512-81-0 This article mentions the following:
In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives, I (R1 = Ph, 4-MeC6H4, 2-O2NC6H4, etc.; R2 = 2-MeOC6H4,3-MeOC6H4, 4-MeOC6H4, 3-EtOC6H4), II (R3 = Ph, 3,5-Cl2-4-NH2Ph; R4 = 3-MeOPh, 3-EtOPh), were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biol. evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog II (R3 = Ph; R4 = 3-EtOC6H4) (IC50 = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization. In the experiment, the researchers used many compounds, for example, 2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0SDS of cas: 105512-81-0).
2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.SDS of cas: 105512-81-0
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica