Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors

Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors

In the current paper, through a convergent multi-step approach, a library of novel indole-phenyltriazole hybrids containing an amide moiety (9a-k) was synthesized. The structural verification of all synthesized molecules was accomplished by CHN and spectral analyses data. These synthesized bi-hetero...

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Published in:Journal of Heterocyclic Chemistry
Main Author: Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
Format: Article
Language:English
Published: HeteroCorporation 2020
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85085113141&doi=10.1002%2fjhet.4006&partnerID=40&md5=f039d79804cdc8136fd9501b90993585
id 2-s2.0-85085113141
spelling 2-s2.0-85085113141
Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
2020
Journal of Heterocyclic Chemistry
57
7
10.1002/jhet.4006
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85085113141&doi=10.1002%2fjhet.4006&partnerID=40&md5=f039d79804cdc8136fd9501b90993585
In the current paper, through a convergent multi-step approach, a library of novel indole-phenyltriazole hybrids containing an amide moiety (9a-k) was synthesized. The structural verification of all synthesized molecules was accomplished by CHN and spectral analyses data. These synthesized bi-heterocyclic derivatives (9a-k) were evaluated for their anti-ulcer potential by inhibitory action against Jack bean urease enzyme and subsequently their structure-activity relationship was perceived. Moreover, these compounds were inspected for cytotoxic profile by hemolytic activity and it was professed that nearly all the synthesized compounds showed low cytotoxicity. In addition, free radical scavenging activity and kinetic analysis were also carried out for these compounds to understand their mode of inhibition. So, it was summated that these derivatives might lead to further research gateways for obtaining better and safe anti-ulcer agents. © 2020 Wiley Periodicals LLC
HeteroCorporation
0022152X
English
Article
author Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
spellingShingle Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
author_facet Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
author_sort Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
title Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
title_short Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
title_full Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
title_fullStr Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
title_full_unstemmed Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
title_sort Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
publishDate 2020
container_title Journal of Heterocyclic Chemistry
container_volume 57
container_issue 7
doi_str_mv 10.1002/jhet.4006
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85085113141&doi=10.1002%2fjhet.4006&partnerID=40&md5=f039d79804cdc8136fd9501b90993585
description In the current paper, through a convergent multi-step approach, a library of novel indole-phenyltriazole hybrids containing an amide moiety (9a-k) was synthesized. The structural verification of all synthesized molecules was accomplished by CHN and spectral analyses data. These synthesized bi-heterocyclic derivatives (9a-k) were evaluated for their anti-ulcer potential by inhibitory action against Jack bean urease enzyme and subsequently their structure-activity relationship was perceived. Moreover, these compounds were inspected for cytotoxic profile by hemolytic activity and it was professed that nearly all the synthesized compounds showed low cytotoxicity. In addition, free radical scavenging activity and kinetic analysis were also carried out for these compounds to understand their mode of inhibition. So, it was summated that these derivatives might lead to further research gateways for obtaining better and safe anti-ulcer agents. © 2020 Wiley Periodicals LLC
publisher HeteroCorporation
issn 0022152X
language English
format Article
accesstype
record_format scopus
collection Scopus
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