Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents was written by Mostofi, Manizheh;Mohammadi Ziarani, Ghodsi;Lashgari, Negar. And the article was included in Bioorganic & Medicinal Chemistry in 2018.Reference of 38220-75-6 This article mentions the following:
A series of benzofuran appended 1,5-benzothiazepine compounds I (R1 = H, 5-Br, 5-NO2, 7-OMe; R2 = 4-OH, 1-naphthyl, 3-indolyl, etc.) was designed, synthesized and evaluated as cholinesterase inhibitors. The biol. assay experiments showed that most of the compounds displayed a clearly selective inhibition for butyrylcholinesterase (BChE), while a weak or no effect towards acetylcholinesterase (AChE) was detected. All analogs exhibited varied BChE inhibitory activity with IC50 value ranging between 1.0 +/- 0.01 and 72 +/- 2.8 μM when compared with the standard donepezil (IC50, 2.63 +/- 0.28 μM). Among the synthesized derivatives, compounds I (R1 = 5-Br; R2 = 2-MeO, 3-MeO, 4-MeO) exhibited the highest BChE inhibition with IC50 values of 1.0, 1.0 and 1.8 μM, resp. The results from a Lineweaver-Burk plot indicated a mixed-type inhibition for compound I (R1 = 5-Br; R2 = 3-MeO) with BChE. In addition, docking studies confirmed the results obtained through in vitro experiments and showed that most potent compounds bind to both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of BChE active site. The synthesized compounds were also evaluated for their in vitro antibacterial and antifungal activities. The results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms and showed high activity against both gram pos. and gram neg. bacteria and fungi. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Reference of 38220-75-6).
1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Reference of 38220-75-6
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem