Synthesis, α-amylase inhibition and molecular docking study of bisindolylmethane sulfonamide derivatives

• Published in: Medicinal Chemistry Research
• Main Author: Taha M.; Noreen T.; Imran S.; Nawaz F.; Chigurupati S.; Selvaraj M.; Rahim F.; Hadiani Ismail N.; Kumar A.; Mosaddik A.; Alghamdi A.M.; Abdulrahman nasser alqahtani Y.; Abdulrahman nasser alqahtani A.
• Format: Article
• Language: English
• Published: Birkhauser Boston 2019
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85071757214&doi=10.1007%2fs00044-019-02431-4&partnerID=40&md5=93c0f889f68b704a14359e94b957c2eb

We have synthesized nineteen (1–19) bisindolylmethane sulfonamide analogs, characterized by different spectroscopic techniques such as 1HNMR and EI-MS and tested for α-amylase inhibitory potential. All compounds showed excellent to moderate degree of α-amylase inhibitory potential with IC50 values ranging between 1.192 ± 0.51 to 3.057 ± 0.18 μM as equated with standard acarbose (IC50 values 0.83 ± 0.36 μM). Among the series, six analogs such as 1, 4, 5, 6, 10, and 14 showed potent α-amylase inhibition with IC50 values 1.747 ± 0.2, 1.208 ± 0.15, 1.192 ± 0.51, 1.858 ± 0.08, 1.358 ± 0.27 and 1.527 ± 0.17 μM, respectively, as equated with standard acarbose. The structure-activity relationship based upon different substituents on phenyl part. Molecular docking studies performed to recognize the binding interaction of the most active compounds. [Figure not available: see fulltext.] © 2019, Springer Science+Business Media, LLC, part of Springer Nature.