Thiadiazole derivatives as New Class of β-glucuronidase inhibitors

Thiadiazole derivatives as New Class of β-glucuronidase inhibitors

Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50 = 2.16 ± 0.01-58.06 ± 1.60 μM as compare to standard d-saccharic acid 1,4-lacton...

Full description

Bibliographic Details
Published in:Bioorganic and Medicinal Chemistry
Main Author: Salar U.; Taha M.; Ismail N.H.; Khan K.M.; Imran S.; Perveen S.; Wadood A.; Riaz M.
Format: Article
Language:English
Published: Elsevier Ltd 2016
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84961126449&doi=10.1016%2fj.bmc.2016.03.020&partnerID=40&md5=77d703360524d538921852b32b015a5b
id 2-s2.0-84961126449
spelling 2-s2.0-84961126449
Salar U.; Taha M.; Ismail N.H.; Khan K.M.; Imran S.; Perveen S.; Wadood A.; Riaz M.
Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
2016
Bioorganic and Medicinal Chemistry
24
8
10.1016/j.bmc.2016.03.020
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84961126449&doi=10.1016%2fj.bmc.2016.03.020&partnerID=40&md5=77d703360524d538921852b32b015a5b
Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50 = 2.16 ± 0.01-58.06 ± 1.60 μM as compare to standard d-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques 1H, 13C NMR, and EIMS. © 2016 Elsevier Ltd. All rights reserved.
Elsevier Ltd
9680896
English
Article
author Salar U.; Taha M.; Ismail N.H.; Khan K.M.; Imran S.; Perveen S.; Wadood A.; Riaz M.
spellingShingle Salar U.; Taha M.; Ismail N.H.; Khan K.M.; Imran S.; Perveen S.; Wadood A.; Riaz M.
Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
author_facet Salar U.; Taha M.; Ismail N.H.; Khan K.M.; Imran S.; Perveen S.; Wadood A.; Riaz M.
author_sort Salar U.; Taha M.; Ismail N.H.; Khan K.M.; Imran S.; Perveen S.; Wadood A.; Riaz M.
title Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
title_short Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
title_full Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
title_fullStr Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
title_full_unstemmed Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
title_sort Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
publishDate 2016
container_title Bioorganic and Medicinal Chemistry
container_volume 24
container_issue 8
doi_str_mv 10.1016/j.bmc.2016.03.020
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84961126449&doi=10.1016%2fj.bmc.2016.03.020&partnerID=40&md5=77d703360524d538921852b32b015a5b
description Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50 = 2.16 ± 0.01-58.06 ± 1.60 μM as compare to standard d-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques 1H, 13C NMR, and EIMS. © 2016 Elsevier Ltd. All rights reserved.
publisher Elsevier Ltd
issn 9680896
language English
format Article
accesstype
record_format scopus
collection Scopus
_version_ 1809677910228860928

Similar Items