2014Unpublished venueRequires access

DESIGN, SYNTHESIS, MOLECULAR DOCKING AND ANTIBACTERIAL EVALUATION OF NOVEL N-(6, 11-DIOXO-DIHYDRO-5H-BENZO (B) CARBAZOL-2YL) BENZAMIDE DERIVATIVES AS POTENT ANTIBACTERIAL AGENTS Original Article

P. Ravi Chandiran, Premnath Dhanaraj, Surender Kumar

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Abstract

Objective: Heterocyclic quinone derivatives are important class of organic compounds both in biological and electrochemical applications. In this article our prime motivation is to develop novel series of heterocyclic quinone derivatives for antibacterial applications. Clinically isolated different Gram-negative and Gram-positive bacterial microorganisms were studied in this article and reported. Methods: A novel series of N-(6,11-dioxo-dihydro-5H-benzo[b]carbazol-2yl) benzamide derivatives were synthesized by the Michael addition of 1,4-naphthoquinone and para-phenylene diamine. The derivatives of compound 1 were synthesized, subjecting it to benzolyation by a variety of acid chlorides. To understand the interaction of binding sites with bacterial protein receptor, the docking study was performed by glide program. In vitro antibacterial activity of the synthesized compounds was studied and the MIC value was calculated by the agar dilution method. Results: The compound 2b (0.4 µg/mL) exhibited good antibacterial activity against staphylococcus aureus than the standards sparfloxacin (4.87 µg/mL) and Norfloxacin (39.06 µg/mL) which was employed. Conclusion: This investigation identified the potent antibacterial agents and these molecules will be subjected to further studies in our laboratory.

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Objective: Heterocyclic quinone derivatives are important class of organic compounds both in biological and electrochemical applications. In this article our prime motivation is to develop novel series of heterocyclic quinone derivatives for antibacterial applications. Clinically isolated different Gram-negative and Gram-positive bacterial microorganisms were studied in this article and reported. Methods: A novel series of N-(6,11-dioxo-dihydro-5H-benzo[b]carbazol-2yl) benzamide derivatives were synthesized by the Michael addition of 1,4-naphthoquinone and para-phenylene diamine. The derivatives of compound 1 were synthesized, subjecting it to benzolyation by a variety of acid chlorides. To understand the interaction of binding sites with bacterial protein receptor, the docking study was performed by glide program. In vitro antibacterial activity of the synthesized compounds was studied and the MIC value was calculated by the agar dilution method. Results: The compound 2b (0.4 µg/mL) exhibited good antibacterial activity against staphylococcus aureus than the standards sparfloxacin (4.87 µg/mL) and Norfloxacin (39.06 µg/mL) which was employed. Conclusion: This investigation identified the potent antibacterial agents and these molecules will be subjected to further studies in our laboratory.

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Available abstract

Objective: Heterocyclic quinone derivatives are important class of organic compounds both in biological and electrochemical applications. In this article our prime motivation is to develop novel series of heterocyclic quinone derivatives for antibacterial applications. Clinically isolated different Gram-negative and Gram-positive bacterial microorganisms were studied in this article and reported. Methods: A novel series of N-(6,11-dioxo-dihydro-5H-benzo[b]carbazol-2yl) benzamide derivatives were synthesized by the Michael addition of 1,4-naphthoquinone and para-phenylene diamine. The derivatives of compound 1 were synthesized, subjecting it to benzolyation by a variety of acid chlorides. To understand the interaction of binding sites with bacterial protein receptor, the docking study was performed by glide program. In vitro antibacterial activity of the synthesized compounds was studied and the MIC value was calculated by the agar dilution method. Results: The compound 2b (0.4 µg/mL) exhibited good antibacterial activity against staphylococcus aureus than the standards sparfloxacin (4.87 µg/mL) and Norfloxacin (39.06 µg/mL) which was employed. Conclusion: This investigation identified the potent antibacterial agents and these molecules will be subjected to further studies in our laboratory.

Key concepts: Chemistry, Benzamide, Antibacterial activity, Docking (animal), Naphthoquinone, Norfloxacin, Combinatorial chemistry, Stereochemistry

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DESIGN, SYNTHESIS, MOLECULAR DOCKING AND ANTIBACTERIAL EVALUATION OF NOVEL N-(6, 11-DIOXO-DIHYDRO-5H-BENZO (B) CARBAZOL-2YL) BENZAMIDE DERIVATIVES AS POTENT ANTIBACTERIAL AGENTS Original Article — Research Paper | ScholarLens