1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.

Autor:	Lu Y; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Mann CA; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Nolan S; Microbial Infection and Immunity, College of Medicine, The Ohio State University, Columbus, Ohio 43210, United States., Collins JA; Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States., Parker E; Department of Veterinary Preventive Medicine, College of Veterinary Medicine, The Ohio State University, Columbus, Ohio 43210, United States., Papa J; Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Vibhute S; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Jahanbakhsh S; Micromyx, Kalamazoo, Michigan 49008, United States., Thwaites M; Micromyx, Kalamazoo, Michigan 49008, United States., Hufnagel D; Micromyx, Kalamazoo, Michigan 49008, United States., Hazbón MH; ATCC, Manassas, Virginia 20110, United States., Moreno J; ATCC, Manassas, Virginia 20110, United States., Stedman TT; ATCC, Manassas, Virginia 20110, United States., Wittum T; Department of Veterinary Preventive Medicine, College of Veterinary Medicine, The Ohio State University, Columbus, Ohio 43210, United States., Wozniak DJ; Microbial Infection and Immunity, College of Medicine, The Ohio State University, Columbus, Ohio 43210, United States.; Department of Microbiology, College of Arts and Sciences, The Ohio State University, Columbus, Ohio 43210, United States., Osheroff N; Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.; Department of Medicine (Hematology/Oncology), Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.; VA Tennessee Valley Healthcare System, Nashville, Tennessee 37212, United States., Yalowich JC; Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Mitton-Fry MJ; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
Jazyk:	angličtina
Zdroj:	ACS medicinal chemistry letters [ACS Med Chem Lett] 2022 May 09; Vol. 13 (6), pp. 955-963. Date of Electronic Publication: 2022 May 09 (Print Publication: 2022).
DOI:	10.1021/acsmedchemlett.2c00111
Abstrakt:	Antibacterial resistance continues its devastation of available therapies. Novel bacterial topoisomerase inhibitors (NBTIs) offer one solution to this critical issue. Two series of amine NBTIs bearing tricyclic DNA-binding moieties as well as amide NBTIs with a bicyclic DNA-binding moiety were synthesized and evaluated against methicillin-resistant Staphylococcus aureus (MRSA). Additionally, these compounds and a series of bicyclic amine analogues displayed high activity against susceptible and drug-resistant Neisseria gonorrhoeae , expanding the spectrum of these dioxane-linked NBTIs. Competing Interests: The authors declare the following competing financial interest(s): M.J.M.-F. is a shareholder of Pfizer. (© 2022 American Chemical Society.)
Databáze:	MEDLINE
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