摘要:
1''-( Beta -Hydroxyethyl)-1''-demethylclindamycin 2-acylate compounds of the formula:
OR THE ACID ADDITION SALTS THEREOF WHEREIN Halo is chlorine, bromine, or iodine, X is an acyl radical of an aliphatic carboxylic acid having from 2 to 18 carbon atoms, inclusive; R is alkyl of not more than 4 carbon atoms; and R1 is alkyl of not more than 8 carbon atoms. The compounds have clindamycin-like antibacterial activity and provide particularly high concentrations of compound in the urinary tract thereby being particularly useful in treating bacterial infections of the upper and lower urinary tract as well as L-forms in the kidney.
摘要:
ALKYL 7-DEXY-7-MERCAPTOALKYLTHIO-A-THIOLINCONSAMINIDES USEFUL AS INTERMEDIATES FOR PREPARING ANTIBACTERIALLY ACTIVE 7-DEOXY-7-MERCAPTOALKYLTHIO-LINCOMYCINS ARE PREPARED BY HEATING ALKYL N-ACYL-6,7-AZIRIDINO-6-DEAMINO-7-DEOXY-ATHIOLINCOSAMINIDES WITH AN APPROPRIATE SULFIDE IN THE PRESENCE OF GLACIAL ACETIC ACID OR OTHER ANHYDROUS LOWER ALKANOIC ACID, OR ANHYDROUS BENZOIC ACID OR OTHER ARENOIC ACID OR NOT MORE THAN 12 CARBON ATOMS.
摘要:
6''-N-alkyl derivatives of kanamycin, 3'',4''-dideoxykanamycin B, 3'',4''-dideoxyneamine and 3'', 4''-dideoxyvistamycin, typically represented by 6''-N-methylkanamycin, 6''-N-methyl-3'',4''dideoxykanamycin B and 6''-N-methyl-3'', 4''-dideoxyvistamycin are synthetized by 6''-N-alkyltalation of the parent substances kanamycin, 3'',4''-dideoxykanamycin B, 3'',4''-dideoxynamine and 3'', 4''-dideoxyvistamycin and are new semi-synthetic antibiotics which are usefully active even against Escherichia and Pseudomonas species resistant to the parent substances.
摘要:
Modified flavonoid glycosides are prepared wherein the molecules include two or more glucose substituents. Such modified flavonoid glycosides exhibit uniquely higher solubilities than the unmodified compounds. Modification is achieved by reacting flavonoid monoglycosides with starchy materials in the presence of Alpha -amylase enzymes. The resultant flavonoid glycosides include principally two or three glucose substituents per molecule. Further reaction of the modified glycosides with Beta -amylase gives rise to decomposition of the glycoside having a high polymerization degree and a flavonoid glycoside having two or three glucoses per molecule is solely obtained.