- INHIBITORS OF METALLO-BETA-LACTAMASE (MBL) COMPRISING A ZINC CHELATING MOIETY
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The invention provides compounds according to formula I: A - L - B wherein A represents a lipophilic chelating moiety which is selective for Zn2+ ions; L is a covalent bond or a linker; and B is a vector which is either a moiety capable of interacting with one or more biological structures found in a bacterium (preferably in a bacterial cell wall), for example a penicillin-binding protein such as a metallo-β- lactamase or DD-transferase, or a moiety capable of enhancing transport of the compound across a bacterial cell membrane. Such compounds find use in a method of treating and/or preventing a bacterial infection in a human or non-human mammal. In such a method, the compound of formula I may be administered in combination with (either simultaneously, separately, or sequentially) a β-lactam antibiotic.
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Page/Page column 43; 44
(2015/04/22)
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- Propargyl-substituted phosphonocarboxylates: Efficient synthesis and application to click chemistry
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An efficient pathway for the selective preparation of monopropargyl- substituted phosphonocarboxylate (PC) has been developed via the addition of sodium, acetylenide to ethylidenephosphonate. The reaction works perfectly on multi-gram scales. The synthesi
- Artyushin, Oleg I.,Osipov, Sergey N.,Roeschenthaler, Gerd-Volker,Odinets, Irina L.
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experimental part
p. 3579 - 3588
(2010/03/30)
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- Synthetic Routes to 1-Substituted Butadienylphosphonates
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The synthesis of 1-substituted butadienylphosphonates 5 was attempted on three routes.The easily polymerizing butadienes are generally accessible from the stable phosphonates 4 by seleninic acid elimination.
- Flitsch, Wilhelm,Rosche, Juergen,Lubisch, , Wilfried
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p. 661 - 664
(2007/10/02)
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- Heterogeneous mediated Alkylation of Ethyl Diethylphosphonoacetate. A "One Pot" Access to α-Alkylated Acrylic Esters
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Ethyl diethylphosphonoacetates are α-alkylated in high yield in a heterogeneous reaction with solid potassium carbonate as base.A "one pot" synthesis of α-alkylated acrylic esters is achiewed in a PO-actived olefination reaction aqueous media, when aqueous potassium carbonate and formaldehyde are added directly to the above reaction mixture.
- Kirschleger, Bernard,Queignec, Rene
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p. 926 - 928
(2007/10/02)
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- A New Synthesis of 5-Methyl-3-methylene-γ-butyrolactone
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An useful synthesis of 5-methyl-3-methylene-γ-butyrolactone (6) involving a Wittig-Horner reaction as a key step is described.
- Ravikumar, V. T.,Swaminathan, S.,Rajagopalan, K.
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p. 292 - 293
(2007/10/02)
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- SYNTHESIS OF ETHYL-α- PROPARGYL ACRYLATE - A USEFUL FIVE CARBON SYNTHON
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The title compound has been synthesised via an alkylation, Wittig-Horner reaction sequence, Michael addition of several active methylene substrates with compound 1 has been carried out.
- Ravikumar, V.T.,Swaminathan, S.,Rajagopalan, K.
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p. 6045 - 6046
(2007/10/02)
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