2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity

Synthesis of 2-(2'-pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro ß-glucuronidase inhibitory potential. The compounds 4 (IC50 = 4.06 ± 0.34 μM), 5 (IC50 = 09.63 ± 0.81 μM), 1 (IC50 = 19.66 ± 0.44 μM), 7 (IC50 = 24.75 ± 0.25 μM), 6 (IC50 = 26.30 ± 1.37 μM),...

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Published in:	Journal of the Chemical Society of Pakistan
Main Author:	Kamil A.; Akhtar S.; Noureen S.; Saify Z.S.; Jahan S.; Khan K.M.; Rahim F.; Taha M.; Mushtaq N.; Arif M.; Perveen S.; Chaudhary M.I.
Format:	Article
Language:	English
Published:	Chemical Society of Pakistan 2015
Online Access:	https://www.scopus.com/inward/record.uri?eid=2-s2.0-84953331043&partnerID=40&md5=a41f6149582721818f824995a58265a8

id	2-s2.0-84953331043
spelling	2-s2.0-84953331043 Kamil A.; Akhtar S.; Noureen S.; Saify Z.S.; Jahan S.; Khan K.M.; Rahim F.; Taha M.; Mushtaq N.; Arif M.; Perveen S.; Chaudhary M.I. 2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity 2015 Journal of the Chemical Society of Pakistan 37 4 https://www.scopus.com/inward/record.uri?eid=2-s2.0-84953331043&partnerID=40&md5=a41f6149582721818f824995a58265a8 Synthesis of 2-(2'-pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro ß-glucuronidase inhibitory potential. The compounds 4 (IC50 = 4.06 ± 0.34 μM), 5 (IC50 = 09.63 ± 0.81 μM), 1 (IC50 = 19.66 ± 0.44 μM), 7 (IC50 = 24.75 ± 0.25 μM), 6 (IC50 = 26.30 ± 1.37 μM), and 3 (IC50 = 32.11 ± 0.89 μM), showed ß-glucuronidase inhibitory activity superior to the standard D-saccharic acid 1,4-lactone, with (IC50 = 48.4 ± 1.25 μM). Based on structure-activity relationship, we discover a new class of potent ß-glucuronidase inhibitors. Chemical Society of Pakistan 02535106 English Article
author	Kamil A.; Akhtar S.; Noureen S.; Saify Z.S.; Jahan S.; Khan K.M.; Rahim F.; Taha M.; Mushtaq N.; Arif M.; Perveen S.; Chaudhary M.I.
spellingShingle	Kamil A.; Akhtar S.; Noureen S.; Saify Z.S.; Jahan S.; Khan K.M.; Rahim F.; Taha M.; Mushtaq N.; Arif M.; Perveen S.; Chaudhary M.I. 2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
author_facet	Kamil A.; Akhtar S.; Noureen S.; Saify Z.S.; Jahan S.; Khan K.M.; Rahim F.; Taha M.; Mushtaq N.; Arif M.; Perveen S.; Chaudhary M.I.
author_sort	Kamil A.; Akhtar S.; Noureen S.; Saify Z.S.; Jahan S.; Khan K.M.; Rahim F.; Taha M.; Mushtaq N.; Arif M.; Perveen S.; Chaudhary M.I.
title	2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
title_short	2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
title_full	2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
title_fullStr	2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
title_full_unstemmed	2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
title_sort	2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity
publishDate	2015
container_title	Journal of the Chemical Society of Pakistan
container_volume	37
container_issue	4
doi_str_mv
url	https://www.scopus.com/inward/record.uri?eid=2-s2.0-84953331043&partnerID=40&md5=a41f6149582721818f824995a58265a8
description	Synthesis of 2-(2'-pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro ß-glucuronidase inhibitory potential. The compounds 4 (IC50 = 4.06 ± 0.34 μM), 5 (IC50 = 09.63 ± 0.81 μM), 1 (IC50 = 19.66 ± 0.44 μM), 7 (IC50 = 24.75 ± 0.25 μM), 6 (IC50 = 26.30 ± 1.37 μM), and 3 (IC50 = 32.11 ± 0.89 μM), showed ß-glucuronidase inhibitory activity superior to the standard D-saccharic acid 1,4-lactone, with (IC50 = 48.4 ± 1.25 μM). Based on structure-activity relationship, we discover a new class of potent ß-glucuronidase inhibitors.
publisher	Chemical Society of Pakistan
issn	02535106
language	English
format	Article
accesstype
record_format	scopus
collection	Scopus
_version_	1820775476728168448

2-(2'-pyridyl) benzimidazole analogs and their ß-glucuronidase inhibitory activity

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