Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study

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...

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Published in:European Journal of Medicinal Chemistry
Main Author: Taha M.; Irshad M.; Imran S.; Chigurupati S.; Selvaraj M.; Rahim F.; Ismail N.H.; Nawaz F.; Khan K.M.
Format: Article
Language:English
Published: Elsevier Masson s.r.l. 2017
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
id 2-s2.0-85032929001
spelling 2-s2.0-85032929001
Taha M.; Irshad M.; Imran S.; Chigurupati S.; Selvaraj M.; Rahim F.; Ismail N.H.; Nawaz F.; Khan K.M.
Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
2017
European Journal of Medicinal Chemistry
141

10.1016/j.ejmech.2017.10.028
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85032929001&doi=10.1016%2fj.ejmech.2017.10.028&partnerID=40&md5=dd50c9fcba76ab67831ba7f3d8094e0c
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
Elsevier Masson s.r.l.
2235234
English
Article
author Taha M.; Irshad M.; Imran S.; Chigurupati S.; Selvaraj M.; Rahim F.; Ismail N.H.; Nawaz F.; Khan K.M.
spellingShingle Taha M.; Irshad M.; Imran S.; Chigurupati S.; Selvaraj M.; Rahim F.; Ismail N.H.; Nawaz F.; Khan K.M.
Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
author_facet Taha M.; Irshad M.; Imran S.; Chigurupati S.; Selvaraj M.; Rahim F.; Ismail N.H.; Nawaz F.; Khan K.M.
author_sort Taha M.; Irshad M.; Imran S.; Chigurupati S.; Selvaraj M.; Rahim F.; Ismail N.H.; Nawaz F.; Khan K.M.
title Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
title_short Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
title_full Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
title_fullStr Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
title_full_unstemmed Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
title_sort Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
publishDate 2017
container_title European Journal of Medicinal Chemistry
container_volume 141
container_issue
doi_str_mv 10.1016/j.ejmech.2017.10.028
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85032929001&doi=10.1016%2fj.ejmech.2017.10.028&partnerID=40&md5=dd50c9fcba76ab67831ba7f3d8094e0c
description 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
publisher Elsevier Masson s.r.l.
issn 2235234
language English
format Article
accesstype
record_format scopus
collection Scopus
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