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In Vitro and In Vivo Antibacterial Activities of a Novel Glycylcycline, the 9-t-Butylglycylamido Derivative of Minocycline (GAR-936)
Overall, TBG-MINO shows antibacterial activity against a wide spectrum of gram-positive and gram-negative aerobic and anaerobic bacteria including strains resistant to other chemotherapeutic agents. Expand
Crystal structures of the two major aggrecan degrading enzymes, ADAMTS4 and ADAMTS5
These structures show that the unliganded and inhibitor‐bound enzymes exhibit two essentially different catalytic‐site configurations: an autoinhibited, nonbinding, closed form and an open, binding form, suggesting that mature aggrecanases exist as an ensemble of at least two isomers, only one of which is proteolytically active. Expand
In vitro and in vivo antibacterial activities of the glycylcyclines, a new class of semisynthetic tetracyclines
The results show that the glycylcyclines have potent in vitro activities against a wide spectrum of gram-positive and gram-negative, aerobic and anaerobic bacteria, including many resistant strains. Expand
Efflux-Mediated Resistance to Tigecycline (GAR-936) in Pseudomonas aeruginosa PAO1
Glycylcyclines are generally inferior substrates for P. aeruginosa efflux pumps than are narrower-spectrum tetracyclines, and their increased susceptibility to tigecycline was specifically associated with loss of MexXY, suggesting drug efflux mediated by MexCD-OprJ. Expand
Tetracycline analogs affecting binding to Tn10-Encoded Tet repressor trigger the same mechanism of induction.
The dimethylamino function may, thus, play a role in triggering the conformational change of TetR necessary for induction, as well as being the most effective inducer tested in this study. Expand
Recent developments in tetracycline antibiotics.
This review will highlight the pertinent advances in the tetracycline field during the last two decades, including recent progress on elucidating the mechanisms of resistance, and the development of novel tetrACYclines to combat bacterial resistance. Expand
In Vitro and In Vivo Activities of Tigecycline (GAR-936), Daptomycin, and Comparative Antimicrobial Agents against Glycopeptide-Intermediate Staphylococcus aureus and Other Resistant Gram-Positive
The data suggest that tigecycline and daptomycin may offer therapeutic options against clinically relevant resistant pathogens for which current alternatives for treatment are limited. Expand
Synthesis and structure-activity relationship of novel glycylcycline derivatives leading to the discovery of GAR-936.
  • P. Sum, P. Petersen
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 17 May 1999
A number of new glycylcyclines were synthesized for structure-activity relationship study, and GAR-936 (TBG-MINO) shows better activity than the previously reported DMG- MINO and DMg-DMDOT. Expand
Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines.
This report describes the discovery of a new generation of tetracycline antibacterial agents, the "glycylcyclines". These agents are notable for their activity against a broad spectrum ofExpand
Analogues of platelet activating factor. 4. Some modifications of the phosphocholine moiety.
Racemic analogues of platelet activating factor (PAF) in which the methylene bridge separating the phosphate and trimethylammonium moieties is altered in length have been prepared and exhibited no detectable hypotensive or platelet aggregating activity. Expand