Andrew G. Myers

Why sulfur is important in lincosamide antibiotics

Kelvin J. Y. Wu, Elena V. Aleksandrova, Paul J. Robinson, Amy E. Benedetto et autres

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Discovery of a fluorinated macrobicyclic antibiotic through chemical synthesis

Ben I. C. Tresco, Kelvin J. Y. Wu, Antonio Ramkissoon, Elena V. Aleksandrova et autres

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Practical Synthesis of Oxepanoprolines

Kelvin J. Y. Wu, Priscilla Liow, Andrew G. Myers

A new, more scalable route for the synthesis of the common oxepanoproline southern fragment of the antibiotic candidates iboxamycin, cresomycin, and BT-33 is presented. A key transformation in the route is a diastereoselective TiCl 4 -mediated conjugate addition of an allylsilane to …

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Practical Synthesis of Macrobicyclic Thiolincosamines

Kelvin J. Y. Wu, Ben I.C. Tresco, Junzhe Xiao, Dominic N. Y. See et autres

Scalable syntheses of the northern macrobicyclic thiolincosamine fragments of two structurally complex antibiotic candidates, BT-33 and cresomycin, are presented. A key transformation in each route is the highly diastereoselective addition of a putative allenylzinc nucleophile to a common Ellman sulfinimine intermediate using …

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Discovery of a broad-spectrum, fluorinated macrobicyclic antibiotic through chemical synthesis

Ben I. C. Tresco, Kelvin J. Y. Wu, Antonio Ramkissoon, Elena Nikolaevna Aleksandrova et autres

We report the discovery through chemical synthesis of BT-33, a fluorinated macrobicyclic oxepanoprolinamide antibiotic. BT-33 potently inhibits the growth of multidrug-resistant clinical isolates of Gram-positive and Gram-negative bacteria and has an extended half-life in vivo relative to its predecessors cresomycin and iboxamycin. …

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Synthetic lincosamides iboxamycin and cresomycin are active against ocular multidrug-resistant methicillin-resistant Staphylococcus aureus carrying erm genes

CAMILLE C. ANDRE, Kelvin J. Y. Wu, Andrew G. Myers, Paulo J. M. Bispo

• New synthetic lincosamides, iboxamycin and cresomycin, display potent in vitro activity against ocular methicillin-resistant Staphylococcus aureus (MRSA) isolates. • Both drugs are active against widespread MRSA clonal complexes CC8 and CC5. • The in vitro potencies of iboxamycin and cresomycin are …

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An antibiotic preorganized for ribosomal binding overcomes antimicrobial resistance

Kelvin J. Y. Wu, Ben I. C. Tresco, Antonio Ramkissoon, Elena V. Aleksandrova et autres

We report the design conception, chemical synthesis, and microbiological evaluation of the bridged macrobicyclic antibiotic cresomycin (CRM), which overcomes evolutionarily diverse forms of antimicrobial resistance that render modern antibiotics ineffective. CRM exhibits in vitro and in vivo efficacy against both Gram-positive and …

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Structural basis of Cfr-mediated antimicrobial resistance and mechanisms to evade it

Elena V. Aleksandrova, Kelvin J. Y. Wu, Ben I. C. Tresco, Egor A. Syroegin et autres

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A case of Scedosporium prolificans pulmonary infection in a patient with acute myeloid leukemia

Abdullah Arjomand, Andrew G. Myers, Padmastuti Akella

An elderly woman with a history of myelodysplastic syndrome complicated by cavitary pneumonia treated with antibiotics and antifungal therapy was admitted with severe sepsis and pulmonary opacities on imaging. Pulmonary infection with Scedosporium prolificans, was diagnosed on bronchopulmonary lavage (BAL). This common …

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Analgesic onset and efficacy of a fast-acting formulation of acetaminophen in a postoperative dental impaction pain model

Andrew G. Myers, Cathy K. Gelotte, Brenda A. Zimmerman, Ami Shenoy et autres

OBJECTIVES: Speed of onset can be critical to an analgesic's efficacy treating acute pain. To enhance onset, a new oral acetaminophen formulation intended to be fast acting was developed. Two studies evaluated the analgesic onset, efficacy, and safety of this fast-acting acetaminophen …

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Structural basis of Cfr-mediated antimicrobial resistance and mechanisms for its evasion

Elena V. Aleksandrova, Kelvin J. Y. Wu, Ben I. C. Tresco, Egor A. Syroegin et autres

ABSTRACT The ribosome is an essential drug target as many classes of clinically important antibiotics bind and inhibit its functional centers. The catalytic peptidyl transferase center (PTC) is targeted by the broadest array of inhibitors belonging to several chemical classes. One of …

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A method for tritiation of iboxamycin permits measurement of its ribosomal binding

Kelvin J. Y. Wu, Dorota Klepacki, Alexander S. Mankin, Andrew G. Myers

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