4.6 Article

Synthesis, molecular docking, antimicrobial, antioxidant and anticonvulsant assessment of novel S and C-linker thiazole derivatives

期刊

CHEMICAL PHYSICS LETTERS
卷 791, 期 -, 页码 -

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ELSEVIER
DOI: 10.1016/j.cplett.2022.139408

关键词

Thiazole; Antimicrobial; Antioxidant; Anticonvulsant; Molecular docking

资金

  1. Department of Basic Science and Technology, Jain University
  2. King Saud University, Riyadh, Saudi Arabia [RSP-2021/78]
  3. Basic Science Research Pro-gram through the National Research Foundation of Korea (NRF) - Ministry of Education [2021R1A6A1A03043682]

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In this study, a multistep reaction sequence was explored to obtain novel anticonvulsant compounds with greater selectivity and reduced toxicity. These compounds exhibited promising antimicrobial and antioxidant activities.
In medicinal chemistry, the searching for new anticonvulsants with greater selectivity and reduced toxicity is still active. Therefore, multistep reaction sequence has been explored to obtained novel series of S and C-linker thiazole derivatives (7a-h and 8a-d). The final compounds were screened for antimicrobial activity against different microbial strains. The DPPH and hydroxyl radical scavenging methods were evaluated to assess their antioxidant capabilities. The anticonvulsant activity was established in MES and PTZ seizure models and the most active compound was 7b and 7 g which showed 100% protection. A computational study was also carried out including drug likeness and docking studies.

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