TY - JOUR
T1 - Synthesis, α-amylase inhibition and molecular docking study of bisindolylmethane sulfonamide derivatives
AU - Taha, Muhammad
AU - Noreen, Tayyaba
AU - Imran, Syahrul
AU - Nawaz, Fasial
AU - Chigurupati, Sridevi
AU - Selvaraj, Manikandan
AU - Rahim, Fazal
AU - Hadiani Ismail, Nor
AU - Kumar, Ashok
AU - Mosaddik, Ashik
AU - Alghamdi, Abdullah M.
AU - Abdulrahman nasser alqahtani, Yousif
AU - Abdulrahman nasser alqahtani, Abdulaziz
N1 - Publisher Copyright:
© 2019, Springer Science+Business Media, LLC, part of Springer Nature.
Copyright:
Copyright 2019 Elsevier B.V., All rights reserved.
PY - 2019/11
Y1 - 2019/11
N2 - 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.]
AB - 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.]
KW - Bisindolylmethane sulfonamide
KW - Molecular docking
KW - SAR
KW - Synthesis
KW - α-Amylase Inhibitory Potential
UR - http://www.scopus.com/inward/record.url?scp=85071757214&partnerID=8YFLogxK
U2 - 10.1007/s00044-019-02431-4
DO - 10.1007/s00044-019-02431-4
M3 - Article
AN - SCOPUS:85071757214
SN - 1054-2523
VL - 28
SP - 2010
EP - 2022
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 11
ER -