Hameed, Shehryar; Kanwal; Seraj, Faiza; Rafique, Rafaila; Chigurupati, Sridevi; Wadood, Abdul; Rehman, Ashfaq Ur; Venugopal, Vijayan; Salar, Uzma; Taha, Muhammad; Khan, Khalid Mohammed published their research in European Journal of Medicinal Chemistry on December 1 ,2019. The article was titled 《Synthesis of benzotriazoles derivatives and their dual potential as α-amylase and α-glucosidase inhibitors in-vitro: Structure-activity relationship, molecular docking and kinetic studies》.Quality Control of 2-Chloro-3,4-difluorobenzoic acid The article contains the following contents:
Benzotriazoles were synthesized which were further reacted with different substituted benzoic acids and phenacyl bromides to synthesize benzotriazole derivatives I [R1 = R2 = H, Me, Cl; R3 = H, 4-Br, 3-Me-4-NO2, etc.] and II [R4 = R5 = H, Me, Cl; R6 = H, 2-OH, 4-Ph, etc.]. The synthetic compounds I and II were characterized via different spectroscopic techniques including EI-MS, HREI-MS, 1H- and 13C-NMR. These mols. were examined for their anti-hyperglycemic potential hence were evaluated for α-glucosidase and α-amylase inhibitory activities. All benzotriazoles displayed moderate to good inhibitory activity in the range of IC50 values of 2.00-5.6 and 2.04-5.72 μM against α-glucosidase and α-amylase enzymes, resp. The synthetic compounds were divided into two categories “”A”” and “”B””, in order to understand the structure-activity relationship. Compounds II [R4 = R5 = H; R6 = 4-Cl] (IC50 = 2.41 ± 1.31 μM), (IC50 = 2.5 ± 1.21 μM), II [R4 = R5 = Me; R6 = 3,4-di-Cl] (IC50 = 2.12 ± 1.35 μM), (IC50 = 2.21 ± 1.08 μM) and II [R4 = R5 = Me; R6 = 4-Cl] (IC50 = 2.00 ± 1.22 μM), (IC50 = 2.04 ± 1.4 μM) with chloro substitution/s at aryl ring were found to be most active against α-glucosidase and α-amylase enzymes. Mol. docking studies on all compounds were performed which revealed that chloro substitutions were playing a pivotal role in the binding interactions. The enzyme inhibition mode was also studied and the kinetic studies revealed that the synthetic mols. showed competitive mode of inhibition against α-amylase and non-competitive mode of inhibition against α-glucosidase enzyme. In the part of experimental materials, we found many familiar compounds, such as 2-Chloro-3,4-difluorobenzoic acid(cas: 150444-93-2Quality Control of 2-Chloro-3,4-difluorobenzoic acid)
2-Chloro-3,4-difluorobenzoic acid(cas: 150444-93-2) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. Quality Control of 2-Chloro-3,4-difluorobenzoic acid The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics