Chen, Xin published the artcileAcetic Acid Derivatives of 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxide as a Novel Class of Potent Aldose Reductase Inhibitors, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Journal of Medicinal Chemistry (2010), 53(23), 8330-8344, database is CAplus and MEDLINE.
A series of novel benzothiadiazine 1,1-dioxide derivatives were synthesized and tested for their inhibitory activity against aldose reductase. Of these derivatives, 17 compounds, having a substituted N2-benzyl group and a N4-acetic acid group on the benzothiadiazine, were found to be potent and selective aldose reductase inhibitors in vitro with IC50 values ranging from 0.032 to 0.975 μM. I (R1=Cl, R2=2,4,5-F3) proved to be the most active in vitro. The eight top-scoring compounds coming from the in vitro test for ALR2 inhibition activity were then tested in vivo, whereby three derivatives, I (R1=F, R2=2,4,5-F3; R1=Cl, R2=2-F,4-Br; R1=Cl, R2=2,4,5-F3) demonstrated a significantly preventive effect on sorbitol accumulation in the sciatic nerve in the 5-day streptozotocin-induced diabetic rats in vivo. Structure-activity relationship and mol. docking studies highlighted the importance of substitution features of N4-acetic acid group and halogen-substituted N2-benzyl group in the benzothiadiazine scaffold and indicated that substitution with halogen at C-7 had a remarkably strong effect on ALR2 inhibition potency.
Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary