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pro vyhledávání: '"John L. Pace"'
Autor:
John L Pace
Publikováno v:
Open Forum Infectious Diseases. 9
Background Fosfomycin (F) inhibits the first committed step of peptidoglycan biosynthesis catalyzed by the MurA enzyme which uses phosphoenolpyruvate as a substrate. Trimethoprim and sulfamethoxazole (TS) inhibit successive steps in folate biosynthes
Publikováno v:
Antimicrobial Agents and Chemotherapy. 59:1931-1934
The novel β-lactamase inhibitor avibactam is a potent inhibitor of class A, class C, and some class D enzymes. The in vitro antibacterial activity of the ceftazidime-avibactam combination was determined for a collection of Enterobacteriaceae clinica
Autor:
Kenneth Coleman, Premavathy Levasseur, Ludovic Lavallade, Christine Miossec, Anne-Marie Girard, John L. Pace
Publikováno v:
Antimicrobial Agents and Chemotherapy. 58:6490-6495
Avibactam is a novel non-β-lactam β-lactamase inhibitor that has been shown in vitro to inhibit class A, class C, and some class D β-lactamases. It is currently in phase 3 of clinical development in combination with ceftazidime. In this study, the
Autor:
John L. Pace, Kevin M. Krause, J. Kevin Judice, Burton G. Christensen, James B. Aggen, Daniel D. Long, Koné Kaniga, Martin S. Linsell, Sharath S. Hegde, Edmund J. Moran
Publikováno v:
The Journal of Antibiotics. 61:595-602
The design, synthesis and antibacterial activity of novel glycopeptide/beta-lactam heterodimers is reported. Employing a multivalent approach to drug discovery, vancomycin and cephalosporin synthons, A and B respectively, were chemically linked to yi
Autor:
John L. Pace, Guang Yang
Publikováno v:
Biochemical Pharmacology. 71:968-980
The natural product glycopeptides vancomycin and teicoplanin have come to play a significant role in the therapy for Gram-positive bacterial infections. In particular vancomycin is the choice for empiric therapy of these infections primarily due to i
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:735-738
A series of lipidated vancomycin analogues 1 bearing disulfide bonds within their lipid chains was designed and synthesized to optimize their ADME profiles while retaining antibacterial potency. These compounds exhibited good activity against resista
Autor:
Kevin M. Krause, Bettina Bazzini, J. Kevin Judice, Burton G. Christensen, Michael R. Leadbetter, Dane E. Karr, Sean G. Trapp, Elizabeth Soriano, Jeng-Pyng Shaw, Paul R. Fatheree, Kelly L. Quast, Lam Bernice M T, Martin S. Linsell, Matthew B. Nodwell, Terry X. Wu, John L. Pace, Jenny D. Villena, Stacy M. Adams
Publikováno v:
The Journal of Antibiotics. 57:326-336
Novel derivatives of N-decylaminoethylvancomycin (2), containing appended hydrophilic groups were synthesized and their antibacterial activity and ADME properties were evaluated. The compounds were prepared by reacting amines with the C-terminus (C-)
Autor:
John L. Pace, Kevin M. Krause, Lesley Farrington, Kelly L. Quast, Martin S. Linsell, Terry X. Wu, Deborah L. Higgins, J. Kevin Judice, Burton G. Christensen, John H. Griffin, Thomas E. Jenkins, Matthew B. Nodwell, Qi-Qi Chen
Publikováno v:
Journal of the American Chemical Society. 125:6517-6531
The design, synthesis, and in vitro microbiological analysis of an array of forty covalently linked vancomycin dimers are reported. This work was undertaken to systematically probe the impact of linkage orientation and linker length on biological act
Autor:
Jessica A. Schuyler, Stacy M. Adams, Dmitri Debabov, Ronald McMillan, Daina Zeng, John L. Pace, Theresa L. Hartsell, Raul J. Cano
Publikováno v:
Cold Spring Harbor Perspectives in Medicine. 6:a026989
The glycopeptide antimicrobials are a group of natural product and semisynthetic glycosylated peptides that show antibacterial activity against Gram-positive organisms through inhibition of cell-wall synthesis. This is achieved primarily through bind
Autor:
Sharath S. Hegde, Matthew B. Nodwell, Martin S. Linsell, Kevin M. Krause, Paul R. Fatheree, Daniel Marquess, David W. Green, John L. Pace, James B. Aggen, Koné Kaniga, Sean G. Trapp, Jason P. Chinn, Seok-Ki Choi, J. Kevin Judice, Burton G. Christensen, Michael R. Leadbetter, S. Derek Turner, Daniel D. Long, Edmund J. Moran
Publikováno v:
The Journal of antibiotics. 61(10)
Further investigations towards novel glycopeptide/beta-lactam heterodimers are reported. Employing a multivalent approach to drug discovery, vancomycin and cephalosporin synthons, 4, 2, 5 and 10, 18, 25 respectively, were chemically linked to yield h