Category: iodides-buliding-blocksIn 2019 ,《Synthesis and exploration of in-silico and in-vitro α-glucosidase and α-amylase inhibitory activities of N-(3-acetyl-2-methyl-4-phenylquinolin-6-yl)arylamides》 appeared in Journal of the Iranian Chemical Society. The author of the article were Kumar, L. Jyothish; Suresh, Y.; Rajasekaran, R.; Reddy, S. Rajeswara; Vijayakumar, V.. The article conveys some information:
Nitro function of 1-(2-methyl-6-nitro-4-phenylquinolin-3-yl)ethanone was converted into amine by grinding it with zinc dust and ammonium chloride which in turn successfully converted into the N-(3-acetyl-2-methyl-4-phenylquinolin-6-yl)arylamides I [R = H, 3-F, 2-O2N, etc.] by treating it with benzoic acids using coupling reagents such as EDC, HATU and DCC. The compounds I were found to afford excellent yields with HATU, moderate in EDC and very less in DCC and hence HATU was considered as a suitable coupling reagent. All the synthesized compounds I were evaluated for their in-silico and in-vitro α-glucosidase and α-amylase inhibitory activity using acarbose as standard to treat type II diabetes and all compounds showed pos. results by in-silico and in-vitro α-amylase inhibition assay. Among the tested compounds, compounds I [R = 2-I, 2-O2N] in α-glucosidase as well as in α-amylase were found to have least binding energy value and form more stable ligand-receptor complex. In addition, the compounds I [R = 2-I, 2-O2N] exhibited 56.90 ± 0.77% and 59.46 ± 0.61% of the higher potent α-glucosidase inhibitory activity with IC50 values 171.75 ± 3.95 μmol/mL and 171.67 ± 1.57 μmol/mL significantly (p < 0.05) compared to remaining seven test samples. And similarly, the compound I [R = 2-I, 2-O2N] possessed α-amylase inhibitory activity at a concentration of 100 μg/mL (55.42 ± 0.42% and 55.42 ± 1.14%) with IC50 values 138.92 ± 4.44 μmol/mL and 158.78 ± 2.34 μmol/mL. In the experiment, the researchers used 2-Iodobenzoic acid(cas: 88-67-5Category: iodides-buliding-blocks)
2-Iodobenzoic acid(cas: 88-67-5) belongs to organic iodides. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Category: iodides-buliding-blocks Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com