Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
Piperazine Sulfonamide analogs (1–19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1–19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when c...
| Published in: | European Journal of Medicinal Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Elsevier Masson s.r.l.
2017
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85032929001&doi=10.1016%2fj.ejmech.2017.10.028&partnerID=40&md5=dd50c9fcba76ab67831ba7f3d8094e0c |
| Summary: | Piperazine Sulfonamide analogs (1–19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1–19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC50 = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2.118 ± 0.204 μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds. © 2017 Elsevier Masson SAS |
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| ISSN: | 2235234 |
| DOI: | 10.1016/j.ejmech.2017.10.028 |