- Synthesis and structure-activity relationships of cephalosporins with C-3' catechol-containing residues
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Cephalosporins with new catechol substituents at C-3' have been synthesized, including novel compounds with C-3' carbon-carbon bonds. Many of these compounds have high potency against Gram-negative bacteria, in particular against resistant strains like Ps
- Arnould,Bertrandie,Bird,Boucherot,Jung,Lohmann,Olivier,Bailey,Bell,Davies
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p. 2631 - 2642
(2007/10/02)
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- Cephalosporin compounds
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Cephalosporin derivatives having a 3-position substituent of the formula I are described: STR1 wherein R1 is hydrogen, alkenyl or optionally substituted alkyl, Het us a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: STR2 wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any adjacent carbon atoms to the benzene ring; and Het being attached to the --CH2 NR1 CO-- group via a carbon atom; R2 is hydroxy or an in vivo hydrolyzable ester thereof; R3 is ortho to R2 and is hydroxy or an in vivo hydrolyzable ester thereof; and R4 has various values. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.
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