An article 2,4-Dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic Acid Derivatives: In Vitro Antidiabetic Activity, Molecular Modeling and In silico ADMET Screening WOS:000458408600007 published article about GLUCOSIDASE INHIBITORY-ACTIVITY; ALPHA-GLUCOSIDASE; BIOLOGICAL EVALUATION; BENZOTHIAZOLE DERIVATIVES; SULFONAMIDE; DOCKING; AMYLASE; BENZENESULFONAMIDE; AGENTS; POTENT in [Thakral, Samridhi; Singh, Vikramjeet] Guru Jambheshwar Univ Sci & Technol, Dept Pharmaceut Sci, Hisar 125001, Haryana, India in 2019, Cited 55. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0. Quality Control of 2,4-Dichlorobenzoic acid
Background: Postprandial hyperglycemia can be reduced by inhibiting major carbohydrate hydrolyzing enzymes, such as alpha-glucosidase and alpha-amylase which is an effective approach in both preventing and treating diabetes. Objective: The aim of this study was to synthesize a series of 2,4-dichloro-5-[(N-and/alkyl)sulfamoyl]benzoic acid derivatives and evaluate alpha-glucosidase and alpha-amylase inhibitory activity along with molecular docking and in silico ADMET property analysis. Method: Chlorosulfonation of 2,4-dichloro benzoic acid followed by reaction with corresponding anilines/amines yielded 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic acid derivatives. For evaluating their antidiabetic potential alpha-glucosidase and alpha-amylase inhibitory assays were carried out. In silico molecular docking studies of these compounds were performed with respect to these enzymes and a computational study was also carried out to predict the drug-likeness and ADMET properties of the title compounds. Results: Compound 3c (2,4-clichloro-5-[(2-nitrophenyl)sulfamoyl]benzoic acid) was found to be highly active having 3 fold inhibitory potential against alpha-amylase and 5 times inhibitory activity against alpha-glucosidase in comparison to standard drug acarbose. Conclusion: Most of the synthesized compounds were highly potent or equipotent to standard drug acarbose for inhibitory potential against alpha-glucosidase and alpha-amylase enzyme and hence this may indicate their antidiabetic activity. The docking study revealed that these compounds interact with active site of enzyme through hydrogen bonding and different pi interactions.
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