- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem -lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar1, Ar2, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 94
(2010/04/06)
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- CARBACEPHEM BETA-LACTAM ANTIBIOTICS
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Carbacephem β-lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, X, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 64
(2010/04/06)
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- CARBACEPHEM BETA-LACTAM ANTIBIOTICS
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Carbacephem β-lactam antibiotics having chemical structures (I) and (II) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R6 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 58
(2010/11/05)
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- Structural modifications and biological evaluation of 3-isoxazolylvinylcephalosporins
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Structural modifications and biological evaluations of 3-isoxazolylvinylcephalosporins (I) were performed. The replacement of a hydrogen atom at the 7-aminothiazole group by a chlorine resulted in an improvement of the activity against resistant Gram-posi
- Pae, Ae Nim,Lee, Jie Eun,Kim, Bo Hyung,Cha, Joo Hwan,Kim, Hea Yeon,Cho, Yong Seo,Choi, Kyung Il,Koh, Hun Yeong,Lee, Eun,Kim, Je Hak
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p. 5657 - 5665
(2007/10/03)
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- Synthesis of HR 916 K: An efficient route to the pure diastereomers of the 1-(pivaloyloxy)ethyl esters of cephalosporins
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HR 916 K (5), the 1-(S)-(pivaloyloxy)ethyl prodrug ester of the cephalosporin cefdaloxime, exhibits a significantly higher oral bioavailability than the 1-(R) diastereomer HR 916 J. An efficient synthesis of HR 916 K was developed. The separation of the diastereomers was achieved by precipitation of the 1-(R)-hydrochloride 9 followed by crystallization of the 1-(S)-amine 10 (de > 96%). The 1-(R) diastereomer 9 was recycled by acidic saponification or enzymatic cleavage to AMCA (7). The amine 10 was acylated with mercaptobenzothiazole thioesters or mixed anhydrides, prepared from carboxylic acids 13 and 14, in almost quantitative yield. Deprotection of the oxime and formation of the tosylate proceeded in one step. Using thioester 18, we obtained HR 916 K (5) from AMCA (7) in 42% yield. VCH Verlagsgesellschaft mbH, 1996.
- Defossa, Elisabeth,Fischer, Gerd,Gerlach, Uwe,Hoerlein, Rolf,Isert, Dieter,Krass, Norbert,Lattrell, Rudolf,Stache, Ulrich,Wollmann, Theo
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p. 1743 - 1749
(2007/10/03)
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