Rational Design of Benzobisheterocycle Metallo-β-Lactamase Inhibitors: A Tricyclic Scaffold Enhances Potency against Target Enzymes

Author:

Villamil Valentina1,Rossi Maria-Agustina2,Mojica Maria F.34,Hinchliffe Philip5ORCID,Martínez Verónica1,Castillo Valerie1,Saiz Cecilia1ORCID,Banchio Claudia26,Macías Mario A.7,Spencer James5ORCID,Bonomo Robert A.348910ORCID,Vila Alejandro246,Moreno Diego M.611ORCID,Mahler Graciela1ORCID

Affiliation:

1. Laboratorio de Química Farmacéutica, Departamento de Química Orgánica, Facultad de Química, Universidad de la República (UdelaR), Avda. General Flores, 2124 Montevideo, Uruguay

2. Instituto de Biología Molecular y Celular de Rosario (IBR, CONICET-UNR), Ocampo y Esmeralda, S2002LRK Rosario, Argentina

3. Department of Molecular Biology and Microbiology, School of Medicine, Case Western Reserve University, 44106 Cleveland, Ohio, United States

4. CWRU-Cleveland VAMC Center for Antimicrobial Resistance and Epidemiology (Case VA CARES), 44106 Cleveland, Ohio, United States

5. School of Cellular and Molecular Medicine, University of Bristol, Biomedical Sciences Building, University Walk, BS8 1TD Bristol, U.K.

6. Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, S2002LRK Rosario, Argentina

7. Crystallography and Chemistry of Materials, CrisQuimMat, Department of Chemistry, Universidad de los Andes, 111711 Bogotá, Colombia

8. Departments of Medicine, Pharmacology, Biochemistry, and Proteomics and Bioinformatics, Case Western Reserve University School of Medicine, 44106 Cleveland, Ohio, United States

9. Research Service, Louis Stokes Cleveland Department of Veterans Affairs Medical Center, 44106 Cleveland, Ohio, United States

10. Clinical Scientist Investigator, Louis Stokes Cleveland Department of Veterans Affairs Medical Center, 44106 Cleveland, Ohio, United States

11. Instituto de Química Rosario (IQUIR, CONICET-UNR), Ocampo y Esmeralda, S2002LRK Rosario, Argentina

Funder

Consejo Nacional de Investigaciones Cient??ficas y T??cnicas

U.S. Department of Health and Human Services

Agencia Nacional de Promoci??n de la Investigaci??n, el Desarrollo Tecnol??gico y la Innovaci??n

Universidad de la Rep??blica Uruguay

Publisher

American Chemical Society (ACS)

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