Zhao, Xuelian; Zhan, Xuehui; Zhang, Huilin; Wan, Yichao; Yang, Huizhong; Wang, Yutian; Chen, Yanda; Xie, Wenlin published their research in Bioorganic & Medicinal Chemistry Letters on December 15 ,2021. The article was titled 《Synthesis and biological evaluation of isatin derivatives containing 1,3,4-thiadiazole as potent a-glucosidase inhibitors》.Reference of 3-Chlorobenzylchloride The article contains the following contents:
A series of isatin derivatives containing 1,3,4-thiadiazole derivatives I [R = 2-F, 3-CN, 4-Cl, etc.] were designed and synthesized. All newly synthesized compounds I were evaluated for their α-glucosidase inhibitory activity with resveratrol as pos. control in-vitro. Except for compounds I [R = 2-CN, 3-CN], all of the compounds I showed a potent inhibitory activity against α-glucosidase with IC50 values in the range of 3.12 ± 1.25 to 45.95 ± 1.26μM and the purity of these compounds were greater than 95%. The IC50 values were being compared to the standard resveratrol (IC50 = 22.00 ± 1.15μM) and it was found that compounds I [R = H, 2-F, 2-Cl, 3-Cl, 4-Cl, 2-Br] were found to be more active than resveratrol. Specifically,I [R = 4-Cl] exhibited the most potent α-glucosidase inhibitory activity with IC50 value of 3.12 ± 1.25μM. The kinetic anal. revealed that compound I [R = 4-Cl] was noncompetitive inhibitor. Structure activity relationship was established for all compounds I. Furthermore, the binding interactions of compound I [R = 4-Cl] with the active site of α-glucosidase were confirmed through mol. docking. This study was identified a new class of potent α-glucosidase inhibitors for further investigation. In the experimental materials used by the author, we found 3-Chlorobenzylchloride(cas: 620-20-2Reference of 3-Chlorobenzylchloride)
3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Reference of 3-Chlorobenzylchloride
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics