- CLPX INHIBITORY COMPOUNDS FOR THE TREATMENT OF MULTI RESISTANT STAPHYLOCOCCUS AUREUS VIRULENCE AND FOR THE TREATMENT OF LEUKEMIA
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The present invention relates to antibiotic compounds and their use as ClpX inhibitors and in the treatment of bacterial infections, such as infections with multi-resistant Staphylococcus aureas, and in the treatment of leukemia. The present invention fur
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Page/Page column 28; 29
(2018/07/26)
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- A Chemical Disruptor of the ClpX Chaperone Complex Attenuates the Virulence of Multidrug-Resistant Staphylococcus aureus
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The Staphylococcus aureus ClpXP protease is an important regulator of cell homeostasis and virulence. We utilized a high-throughput screen against the ClpXP complex and identified a specific inhibitor of the ClpX chaperone that disrupts its oligomeric sta
- Fetzer, Christian,Korotkov, Vadim S.,Th?nert, Robert,Lee, Kyu Myung,Neuenschwander, Martin,von Kries, Jens Peter,Medina, Eva,Sieber, Stephan A.
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p. 15746 - 15750
(2017/10/20)
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- Iridium-catalyzed C-H activation versus directed ortho metalation: Complementary borylation of aromatics and heteroaromatics
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Systematic studies are presented demonstrating the complementarity of directed ortho metalation (DoM) and Ir-catalyzed strategies for the provision of borylated aromatics and their subsequent Suzuki-Miyaura coupling reactions. A new concept, the use of the TMS group, readily introduced by DoM, as a latent regiodirective moiety to overcome the otherwise problematic production of isomeric borylated product mixtures is presented. Additional electrophile-induced ipso-deborylation and DoM reactions of the Bpin products are described.
- Hurst, Timothy E.,Macklin, Todd K.,Becker, Maike,Hartmann, Eduard,Kuegel, Wolfgang,Parisienne-LaSalle, Jean-Christophe,Batsanov, Andrei S.,Marder, Todd B.,Snieckus, Victor
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supporting information; experimental part
p. 8155 - 8161
(2010/09/18)
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- Mutasynthesis of Glycopeptide Antibiotics: Variations of Vancomycin's AB-Ring Amino Acid 3,5-Dihydroxyphenylglycine
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In the mutasynthetic approach, the ΔdpgA mutant of the vancomycin-type glycopeptide antibiotic producer Amycolatopsis balhimycina, which is deficient in the synthesis of 3,5-dihydroxyphenylglycine (DPg), was supplemented with synthetic DPg analogues to obtain the corresponding modified glycopeptides. Sterically more demanding 3,5-disubstituted methoxy derivatives as well as monosubstituted DPg analogues were accepted as substrates. These facts indicate that steric and electronic requirements suffice in several cases for the oxidative closure of the AB ring, thus leading to the generation of novel antibiotically active glycopeptide derivatives. The results represent a further step in evaluating the potential of mutasynthesis for peptidic secondary metabolites. Copyright
- Weist, Stefan,Kittel, Claudia,Bischoff, Daniel,Bister, Bojan,Pfeifer, Volker,Nicholson, Graeme J.,Wohlleben, Wolfgang,Suessmuth, Roderich D.
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p. 5942 - 5943
(2007/10/03)
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- Antineoplastic agents. 465. Structural modification of resveratrol: Sodium resverastatin phosphate
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As an extension of structure/activity investigations of resveratrol (1), phenstatin (2c), and the cancer antiangiogenesis drug sodium combretastatin A-4 phosphate (2b), syntheses of certain related stilbenes (14) and benzophenones (16) were undertaken. The trimethyl ether derivative of (Z)-resveratrol (4a) exhibited the strongest activity (GI50 = 0.01-0.001 μg/mL) against a minipanel of human cancer cell lines. A monodemethylated derivative (14c) was converted to prodrug 14n (sodium resverastatin phosphate) for further biological evaluation. The antitubulin and antimicrobial activities of selected compounds were also evaluated.
- Pettit, George R.,Grealish, Matthew P.,Jung, M. Katherine,Hamel, Ernest,Pettit, Robin K.,Chapuis, J.-Charles,Schmidt, Jean M.
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p. 2534 - 2542
(2007/10/03)
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