PURPOSE: To provide a novel compound useful as a medicine, esp. an antibacterial agent for methicillin-resistant Staphylococcus aureus.
CONSTITUTION: The compound of formula I (R is H, negative electric charge or ester residue; X is S, O or NH; Y is O, NH or H2), e.g. (1R,5S,6 S)-2-{[(Z)-3-(3,4-dihydro-2H-pyrido[4,3-b]-,4-thiazine-6-thio)-1-propenyl]thio}-6-[(R)-1- hydroxyethyl)-1-methylcarbapen-2-em-3-carboxylate. The compound of the formula I can be obtained by reaction of a compound of formula II (R' is carboxyl- protecting group) with a phosphoric esterifying agent or sulfonic esterifying agent followed by substitution reaction with an amine reagent and then eliminating the protecting group. The compound of the present invention also provides excellent activity against both Gram-positive and Gram-negative bacteria, is stable to dehydropeptidase in the kidney, and can be used not as, an agent combined with a dehydropeptidase inhibitor such as cilastatin but as a single agent.
KOIDE TOKUO
NAKAI HIDEKAZU
YOKOTA MASAKI
ARAKI TOMIO
MURAKAMI TAKESHI
NOHARA CHIEKO
