ANTIBIOTIC DERIVATIVES OF GENTAMICIN C1A

1444733 N-Acylated gentamicin C 1a derivatives BRISTOL-MYERS CO 6 Nov 1973 [6 Nov 1972] 51505/73 Heading C2C Novel gentamicin C 1a having at least one amino group acylated with an L-(-)-γ-amino-α- hydroxybutyryl group, and pharmaceutically acceptable acid addition salts and hydrates thereof are prep...

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Bibliographische Detailangaben
Hauptverfasser:	NAITO T,JA, NAKAGAWA S,JA, ABE Y,JA
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOIDCHEMISTRY CHEMISTRY DERIVATIVES THEREOF HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PERFORMING OPERATIONS PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS THEIR RELEVANT APPARATUS TRANSPORTING
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Zusammenfassung:	1444733 N-Acylated gentamicin C 1a derivatives BRISTOL-MYERS CO 6 Nov 1973 [6 Nov 1972] 51505/73 Heading C2C Novel gentamicin C 1a having at least one amino group acylated with an L-(-)-γ-amino-α- hydroxybutyryl group, and pharmaceutically acceptable acid addition salts and hydrates thereof are prepared by blocking the amino group on the 61-carbon atom of gentamicin C 1a with an amino-protective group Y, acylating the resulting novel amino-protected gentamicin C 1a with an L-(-)WNH(CH 2 ) 2 CH(OH)CO- group, wherein W is an amino-protective group and removing Y and W from the resulting amino-protected acylated gentamicin C 1a (also novel when the 1-amino function only of the amino-protected gentamicin C 1a is acylated), and optionally converting the product to a pharmaceutically acceptable acid addition salt or hydrate thereof. Pharmaceutical compositions having antibacterial activity comprise, as active ingredient, gentamicin C 1a the 1-amino function of which is monoacylated with an L-(-)-γ-amino-α-hydroxybutyryl group or a pharmaceutically acceptable acid addition salt or hydrate thereof, together with a pharmaceutically acceptable carrier.