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Design, Synthesis, Biological Screening and Molecular Docking Studies of Novel Multifunctional 1,4-Di (Aryl/heteroaryl) Substituted Piperazine Derivatives as Potential Antitubercular and Antimicrobial Agents by Bruktawit Mekonnen Sanka; Dereje Mamo Tadesse; Endale Teju Bedada; Ephriem T. Mengesha; Neelaiah Babu G. is a Chemistry article available to read on EtoBox.
What is Design, Synthesis, Biological Screening and Molecular Docking Studies of Novel Multifunctional 1,4-Di (Aryl/heteroaryl) Substituted Piperazine Derivatives as Potential Antitubercular and Antimicrobial Agents about?
In this paper, two series of novel multifunctional 1, 4-di (aryl/heteroaryl) substituted piperazine derivatives (6ad & 7a-d) were synthesized, characterized, and evaluated for their antitubercular, antibacterial, and antifungal activities. A step-wise reduction, bromination and substitution reactions on various aldehydes resulted in alcohols (2a-d), bromides (3a-d), and titled novel compounds (6a-d & 7a-d) in moderate to good yields (48-85%). The novel compounds were evaluated for their antitubercular and antimicrobial activities. Compound 7a exhibited promising antitubercular activity (MIC: 0.65 μg/mL) almost equal to the Rifampicin, while the rest of the compounds were moderately active against MTB H37Rv except 6b. Compounds 7a and 6b showed good activity against tested fungal pathogens. Compounds 7a and 7b were proven as the best bacterial agents. Molecular docking studies were in agreement with the in-vitro results. Docking analyses show that all the synthesized molecules bind to the target protein Mtb RNAP (PDB ID: 5UHC) fairly strongly. All the compounds were evaluated for their in vitro cytotoxicity effect using the MTT assay method against human cancer cell line MCF-7. The
Who reads Design, Synthesis, Biological Screening and Molecular Docking Studies of Novel Multifunctional 1,4-Di (Aryl/heteroaryl) Substituted Piperazine Derivatives as Potential Antitubercular and Antimicrobial Agents?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Bruktawit Mekonnen Sanka; Dereje Mamo Tadesse; Endale Teju Bedada; Ephriem T. Mengesha; Neelaiah Babu G.
- Publisher
- Elsevier BV
- Published
- 2021
- Language
- EN
- Field
- Chemistry (Physical Sciences)