Research Journal of Pharmacy and Technology

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Synthesis, Antimicrobial Evaluation and Docking Studies of Novel 4- Acetamido-3-Aminobenzoic Acid Derivatives As Microbial Neuraminidase Inhibitors


Affiliations
1 Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur - 495009, Chhattisgarh, India
     

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Background: Neuraminidase has been considered as vital target for neuraminidase inhibitors (NAI) and designing drug against influenza like new virus strains. The objectives of research work is to synthesized novel 4-acetamido-3-(benzylideneamino)benzoic acid derivatives against microbial neuraminidase (NA) enzyme. Methods: The series of Imine/Schiff base compound were synthesized by reaction of various aldehydes with 4- acetamido-3-amino benzoic acid. Compounds were characterized by IR, 1H NMR and, 13C NMR. Evaluation of synthesized compounds was done against neuraminidase contained bacterial as well as fungal strains. Results: The Compounds 5k-5q, 5x and 5y of novel 4-acetamido-3-aminobenzoic acid derivatives were characterized as potent inhibitory action against the NA contained microbes. The zone of inhibition of these compounds at 125 μg/ml was found (16 ± 2.5), which is more than the standard compounds. Molecular docking of synthesized compounds 5k to 5q showed the highest docking score (> -9 Kj/mol). Conclusion: The compounds 5k-5q, 5x and 5y of novel 4-acetamido-3-aminobenzoic acid derivatives displayed potential neuraminidase inhibition against NA containing microbes. The molecular docking studies predict their binding mode interaction of NA inhibitor. These studies may be further employed, against the neuraminidase contained flu.

Keywords

Antimicrobial, Influenza, Molecular Modeling, Neuraminidase, Para-Amino Benzoic Acid, Schiff Base.
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  • Synthesis, Antimicrobial Evaluation and Docking Studies of Novel 4- Acetamido-3-Aminobenzoic Acid Derivatives As Microbial Neuraminidase Inhibitors

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Authors

Mukesh Kumar Gupta
Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur - 495009, Chhattisgarh, India

Abstract


Background: Neuraminidase has been considered as vital target for neuraminidase inhibitors (NAI) and designing drug against influenza like new virus strains. The objectives of research work is to synthesized novel 4-acetamido-3-(benzylideneamino)benzoic acid derivatives against microbial neuraminidase (NA) enzyme. Methods: The series of Imine/Schiff base compound were synthesized by reaction of various aldehydes with 4- acetamido-3-amino benzoic acid. Compounds were characterized by IR, 1H NMR and, 13C NMR. Evaluation of synthesized compounds was done against neuraminidase contained bacterial as well as fungal strains. Results: The Compounds 5k-5q, 5x and 5y of novel 4-acetamido-3-aminobenzoic acid derivatives were characterized as potent inhibitory action against the NA contained microbes. The zone of inhibition of these compounds at 125 μg/ml was found (16 ± 2.5), which is more than the standard compounds. Molecular docking of synthesized compounds 5k to 5q showed the highest docking score (> -9 Kj/mol). Conclusion: The compounds 5k-5q, 5x and 5y of novel 4-acetamido-3-aminobenzoic acid derivatives displayed potential neuraminidase inhibition against NA containing microbes. The molecular docking studies predict their binding mode interaction of NA inhibitor. These studies may be further employed, against the neuraminidase contained flu.

Keywords


Antimicrobial, Influenza, Molecular Modeling, Neuraminidase, Para-Amino Benzoic Acid, Schiff Base.

References