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Communication

Trifluoromethylated Quinolone-Hydantoin Hybrids: Synthesis and Antibacterial Evaluation

1
Department of Applied Sciences, The NorthCap University, Gurugram 122017, India
2
Department of Translational Research, Western University of Health Sciences, Pomona, CA 91766, USA
3
Department of Pharmacology, College of Medicine, Penn State University, Hershey, PA 17033, USA
4
Department of Natural and Applied Science, University of Dubuque, Dubuque, IA 52001, USA
*
Authors to whom correspondence should be addressed.
Academic Editor: Artur M. S. Silva
Received: 1 June 2022 / Revised: 3 July 2022 / Accepted: 7 July 2022 / Published: 18 July 2022
(This article belongs to the Special Issue Research Progress in Bioorganic Medicinal Chemistry)
A series of new trifluoromethyl-substituted quinolones and hydantoin hybrids has been synthesized and evaluated against Gram-positive bacterium (Staphylococcus aureus MTCC 96) and Gram-negative bacteria (Pseudomonas aeruginosa MTCC 441, Klebsiella pneumonia MTCC 109, and Escherichia coli MTCC 442). Compound  19c, having the 6-propene group on the quinolone ring, showed similar activity to a standard drug (chloramphenicol) by exhibiting MIC values of 50 µg/mL against S. aureus and P. aeruginosa. Physicochemical properties of compound 19c were also determined, which were in line with Lipinski’s rule of five, suggesting the suitability of compound 19c in biological systems. Various types of binding interactions of 19c within the active site of DNA gyrase of S. aureus were also streamlined by molecular docking studies, suggesting its capability to block the catalytic process of the DNA gyrase, which could be the possible reason for its antibacterial potential. View Full-Text
Keywords: quinolones; hydantoin; hybrids; synthesis; antibacterial activity; molecular docking quinolones; hydantoin; hybrids; synthesis; antibacterial activity; molecular docking
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MDPI and ACS Style

Mahajan, A.; Singh, H.; Singh, A.; Agrawal, D.K.; Arora, A.; Chundawat, T.S. Trifluoromethylated Quinolone-Hydantoin Hybrids: Synthesis and Antibacterial Evaluation. Sci 2022, 4, 30. https://doi.org/10.3390/sci4030030

AMA Style

Mahajan A, Singh H, Singh A, Agrawal DK, Arora A, Chundawat TS. Trifluoromethylated Quinolone-Hydantoin Hybrids: Synthesis and Antibacterial Evaluation. Sci. 2022; 4(3):30. https://doi.org/10.3390/sci4030030

Chicago/Turabian Style

Mahajan, Akhil, Harbinder Singh, Amandeep Singh, Devendra K. Agrawal, Amandeep Arora, and Tejpal Singh Chundawat. 2022. "Trifluoromethylated Quinolone-Hydantoin Hybrids: Synthesis and Antibacterial Evaluation" Sci 4, no. 3: 30. https://doi.org/10.3390/sci4030030

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