Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer’s disease was written by Kurt, Belma Zengin;Gazioglu, Isil;Basile, Livia;Sonmez, Fatih;Ginex, Tiziana;Kucukislamoglu, Mustafa;Guccione, Salvatore. And the article was included in European Journal of Medicinal Chemistry in 2015.Electric Literature of C10H7BrO2 This article mentions the following:
The new benzofuranylthiazole derivatives containing the aryl-urea I [R = H, Br, NO2; R1 = H, 2-NO2, 3-OCH3, 4-CH3, etc.] moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds I were assayed. The result showed that all the synthesized compounds I exhibited inhibitory activity on both AChE and BuChE with I [R = Br; R1 = 2-F] (IC50 value of 3.85 μM) and I [R = NO2; R1 = 4-I] (IC50 value of 2.03 μM) as the strongest inhibitors against AChE and BuChE, resp. The compound I [R = NO2; R1 = 4-I] was 8.5-fold more potent than galanthamine. The selectivity index of I [R = Br, NO2; R1 = 2-F, 4-I] was 2.40 and 0.37 against AChE and BuChE, resp. The compound I [R = H; R1 = 3-OCH3, 4-CH3, 4-F] (IC50 = 0.2, 0.5 and 1.13 μM, resp.) showed a better ABTS cation radical scavenging ability than the standard quercetin (IC50 = 1.18 μM). Best poses of compounds I [R = NO2; R1 = 4-I] on BuChE and I [R = Br; R1 = 2-F] on AChE indicate that the thiazole ring and the amidic moiety are important sites of interaction with both ChEs. In addition, the benzofuran ring and Ph ring are anchored to the side chains of both enzymes by π-π interactions. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Electric Literature of C10H7BrO2).
1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Electric Literature of C10H7BrO2
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem