Cephalosporin compounds and antibacterial drugs containing the same
AssigneeEisai Co., Ltd.
InventorsYoshimasa Machida, Isao Saito, Seiichiro Nomoto, Shigeto Negi, Takeo Kanai, Kyosuke Kitoh, Kanemasa Katsu, Yukio Ohya, Takeshi Nagasu
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Abstract
Novel cephalosporin compounds of the general formula: ##STR1## wherein R.sub.1 represents a substituted or unsubstituted nitrogen-containing heterocyclic-thio group, R.sub.2 represents hydrogen or hydroxy, and R.sub.3, R.sub.4 and R.sub.5 each represents hydrogen, hydroxy or acyloxy, and their salts, and processes for the preparation thereof. The novel compounds and their salts have antibacterial activity.
Claims18
A cephalosporin compound of the formula:
- ##STR7## wherein R.sub.1 represents a nitrogen-containing heterocyclic-thio group, the nitrogen-containing heterocyclic group of which is selected from the group consisting of pyrrolyl, pyridyl and its N-oxide, imidazolyl, pyrazolyl, pyrimidinyl, pyridazinyl, 1H-1,2,4-triazolyl, 4H-1,2,4-triazolyl, 1H-1,2,3-triazolyl, 2H-1,2,3-triazolyl, 1H-tetrazolyl, 2H-tetrazolyl, thiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, oxazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, morpholino, benzothiazolyl, and benzoxazolyl, said heterocyclic groups being unsubstituted or substituted by methyl, ethyl, propyl, isopropyl, amino, dimethylaminoethyl, dimethylaminomethyl, diethylaminoethyl, carboxymethyl or carboxyethyl, R.sub.2 represents hydrogen or hydroxy, and R.sub.3, R.sub.4 and R.sub.5 each represents hydrogen, hydroxy, acetoxy, propionyloxy or benzyloxy or a pharmaceutically acceptable salt thereof.
An antibacterial composition which comprises an antibacterially effective amount of a cephalosporin compound of the formula ##STR8## wherein R.sub.1 represents a nitrogen-containing heterocyclic-thio group, the nitrogen-containing heterocyclic group of which is selected from the group consisting of pyrrolyl, pyridyl and its N-oxide, imidazolyl, pyrazolyl, pyrimidinyl, pyridazinyl, 1H-1,2,4-triazolyl, 4H-1,2,4-triazolyl, 1H-1,2,3-triazolyl, 2H-1,2,3-triazolyl, 1H-tetrazolyl, 2H-tetrazolyl, thiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, oxazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, morpholino, benzothiazolyl and benzoxazolyl, said heterocyclic groups being unsubstituted or substituted by methyl, ethyl, propyl, isopropyl, amino, dimethylaminoethyl, dimethylaminomethyl, diethylaminoethyl, carboxymethyl or carboxyethyl, R.sub.2 represents hydrogen or hydroxy, and R.sub.3, R.sub.4 and R.sub.5 each represents hydrogen, hydroxy, acetoxy, propionyloxy or benzyloxy or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Dependencies are inferred from the claim text.