Synthesis of Indole Based Sulfonamide Derivatives as potent inhibitors of α-glucosidase and α-amylase in management of type-II diabetes

• Published in: Chemical Data Collections
• Main Author: Ullah W.; Rahim F.; Hayat S.; Ullah H.; Taha M.; Khan S.; Khaliq A.; Bibi S.; Gohar O.; Iqbal N.; Shah S.A.A.; Khan K.M.
• Format: Data paper
• Language: English
• Published: Elsevier B.V. 2024
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85185155619&doi=10.1016%2fj.cdc.2024.101122&partnerID=40&md5=387a1e0f2244a8a5519f954de0659ea7

We have synthesized indole-based sulfonamides derivatives (1–10), characterized through NMR and HR-EIMS, and screened against α-glucosidase and α-amylase enzymes. All the synthesized analogues showed various degrees of inhibitory potential ranging between 1.10 ± 0.10 to 10.90 ± 0.20 µM (against α-glucosidase) and 0.70 ± 0.10 to 11.30 ± 0.20 µM (against α-amylase) as compared to standard acarbose (IC50 = 38.45 ± 0.10 µM and 1.70 ± 0.10 μM, respectively). In both cases, analogues 5 (IC50 = 1.10 ± 0.10 and 0.40 ± 0.10 μM) and 8 (IC50 = 1.20 ± 0.10 and 0.70 ± 0.10 μM) were identified as the most potent among the series. A structure-activity relationship has been established, which mainly depends upon the substitution pattern around the phenyl ring. The interaction of the most potent analogs with the active site of enzymes was determined through a molecular docking study. © 2024 Elsevier B.V.