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 |
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| Authors: | Wajiha Khan Muhammad A Abbasi Aziz-ur Rehman Sabahat Z Siddiqui Majid Nazir Syed A Ali Shah Hussain Raza Mubashir Hassan Muhammad Shahid Sung Y Seo |
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| Institution: | 1. Department of Chemistry, Government College University, Lahore, Pakistan;2. Faculty of Pharmacy and Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), University Technology MARA, Shah Alam, Malaysia;3. Department of Biological Sciences, College of Natural Sciences, Kongju National University, Gongju, South Korea;4. Institute of Molecular Biology and Biotechnology, The University of Lahore, Lahore, Pakistan;5. Department of Biochemistry, University of Agriculture, Faisalabad, Pakistan |
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| Abstract: | 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. |
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