.beta.-Lactamase inhibitor EM4615
AssigneeE. R. Squibb & Sons, Inc.
InventorsRichard B. Sykes, J. Scott Wells, Pacifico A. Principe, Wen C. Liu
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Abstract
A substance which inhibits the enzyme .beta.-lactamase, produced by a wide range of microorganisms, is obtained when species of the microorganism Micromonospora are cultivated under aerobic fermentation conditions and this inhibitor can be isolated from the fermentation medium by extraction. This substance, denominated EM4615, is useful to enhance the effectiveness of .beta.-lactam antibiotics such as penicillins and cephalosporins.
Claims10
A process for producing the .beta.-lactamase inhibitor EM 4615 which comprises cultivating a Micromonospora species capable of producing the .beta.-lactamase inhibitor in an aqueous nutrient medium comprising an assimilable carbohydrate and an assimilable nitrogen source under submerged aerobic conditions until substantial .beta.-lactamase inhibiting activity is imparted to the medium, and then recovering EM4615.
A process for producing .beta.-lactamase inhibitor EM4615 which comprises cultivating Micromonospora species capable of producing the .beta.-lactamase inhibitor in an aqueous nutrient medium comprising an assimilable carbohydrate and an assimilable nitrogen source under submerged aerobic conditions for about 48 to 240 hours, separating the solids from the fermentation broth, extracting the remaining broth with a lower alkanol at about pH 2, and back extracting the alkanol extract at about pH 7 to 9.
.beta.-lactamase inhibitor EM4615, and salts thereof, said EM4615 having an infrared spectrum, as the sodium salt, as in FIG. 1;
- having the following approximate elemental analysis as the sodium salt:
- C,49.99%;
- H,7,71%;
- O,23.69%;
- S,10.51%;
- Na,8.10%;
- the barium salt thereof melts in the range of about 144.degree.-146.degree. C., the sodium salt thereof is soluble in water and methanol and insoluble in acetone and chloroform;
- the barium salt thereof is soluble in dimethylsulfoxide and dimethylformamide and insoluble in water, methanol, acetone and chloroform.
Dependencies are inferred from the claim text.