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 inJournal of heterocyclic chemistry Vol. 57; no. 7; pp. 2955 - 2968
Main Authors Khan, Wajiha, Abbasi, Muhammad A., Rehman, Aziz‐ur, Siddiqui, Sabahat Z., Nazir, Majid, Ali Shah, Syed A., Raza, Hussain, Hassan, Mubashir, Shahid, Muhammad, Seo, Sung Y.
Format Journal Article
LanguageEnglish
Published Chichester, UK John Wiley & Sons, Inc 01.07.2020
Wiley
Wiley Subscription Services, Inc
Subjects
Chemical synthesis
Chemistry
Chemistry, Organic
Convergence
Derivatives
Free radicals
Hybrid bearings
Jack beans
Physical Sciences
Scavenging
Science & Technology
Toxicity
Ulcers
JACK BEAN UREASE
DESIGN
ANTIUREASE
ANTIOXIDANT ACTIVITIES
DOCKING
OXADIAZOLE SCAFFOLDS
KINETIC MECHANISM
ANTIBACTERIAL
CHEMISTRY
DERIVATIVES
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Summary: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.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.4006