ALPHA-SUBSTITUTED UREIDOBENZYLPENICILLANIC ACID

NEW MATERIAL:A compound of formulaI[R is H or OH; X is n-5C alkyl; Y is group of -(OR )m (R is H, 1-4C lower alkyl, 2-4C lower alkanoyl, etc; m is 1, 2 or 3), group -CN, -COOR (R is H or 1-4C lower alkyl), etc.; n is 2 when Y is -(OR )m, and 1 when Y is another group]and a pharmacologically acceptab...

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Hauptverfasser: KUROKI TOSHIO, SHINOZAKI TEIZOU, MATSUNAGA ISAO, OOI NOBUHIRO, NOFUJI TAKAO, MORO KANJI, NEHASHI TOSHIYUKI, OKAZAKI HIROSHI, SHINDOU MINORU, MATSUMOTO MASAHIKO, ENDOU HISAO, KOJIMA KANA, AOKI BUNYA, KIMURA TAKAO, OGAWA HARUKI, HARADA YUUSUKE
Format: Patent
Sprache:eng
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Zusammenfassung:NEW MATERIAL:A compound of formulaI[R is H or OH; X is n-5C alkyl; Y is group of -(OR )m (R is H, 1-4C lower alkyl, 2-4C lower alkanoyl, etc; m is 1, 2 or 3), group -CN, -COOR (R is H or 1-4C lower alkyl), etc.; n is 2 when Y is -(OR )m, and 1 when Y is another group]and a pharmacologically acceptable salt thereof. EXAMPLE:6-{D(-)-alpha-[3-(3,4-Dihydroxybenzoyl)-3-(3-hydroxypropyl)-1- ureido]- alpha-phenylacetamide}penicillanic acid. USE:An antimicrobial agent capable of exhibiting the activity in the living body particularly on some kinds of microorganisms belonging to the genus Pseudomonas. PROCESS:A novel compound of formula II (R is H, OH, etc.; R is OH, etc.) or a reactive derivative, e.g. pivalic acid or trichloroacetic acid, is reacted with a compound of formula III (R is H or protecting group) or a reactive derivative thereof, and the protecting group is then removed to give the aimed compound of formulaI.