摘要:
Caprazene-1"'-ester derivatives of the formula (III)
wherein Me is methyl group, R 2 is a straight chain or a substantially straight chain alkyl group of 5-21 carbon atoms or a straight chain or a substantially straight chain alkenyl group of 5-21 carbon atoms or an alkynyl group of 5-21 carbon atoms and A is hydrogen atom or an amino-protecting group which is an alkoxycarbonyl group or an aralkyloxycarbonyl group, or a pharmaceutically acceptable acid addition salt thereof. The novel caprazene derivatives exhibit excellent antibacterial activities against a variety of bacteria including acid-fast bacteria.
摘要:
A caprazene-1"'-amide derivative and its 5"-N-alkoxycarbonyl or aralkyloxycarbonyl derivative which are represented by the following general formula (II)
wherein Me is methyl group, R 1 is a straight chain or a substantially straight chain alkyl group of 5-21 carbon atoms, a straight chain or a substantially straight chain alkenyl group of 5-21 carbon atoms or a cycloalkyl group of 5-12 carbon atoms, or R 1 is a phenyl group having a straight chain alkyl group of 1-14 carbon atoms or a straight chain alkoxy group of 1-9 carbon atoms or a cycloalkyl group of 5-12 carbon atoms at the para-position of the phenyl group, A is hydrogen atom or A is an amino-protecting group including an alkoxycarbonyl group, particularly tert-butoxycarbonyl group, or an aralkyloxycarbonyl group, particularly benzyloxycarbonyl group, or a pharmaceutically acceptable acid addition salt thereof
摘要:
Caprazol-1"'-amide derivatives of the formula (V) and caprazol-1"'- amide-3"'-ester derivatives from caprazol. The novel caprazol derivatives now synthesized exhibit excellent antibacterial activities against a variety of bacteria including acid-fast bacteria.
摘要:
Caprazol-3"'-ester derivatives of the formula (VII) wherein Me is methyl group, R 4 is a straight chain or a substantially straight chain alkyl group of 5-21 carbon atoms or a straight chain or a substantially straight chain alkenyl group of 5-21 carbon atoms or an alkynyl group of 5-21 carbon atoms and R 5 is hydrogen atom or an alkyl group of 1-21 carbon atoms, or a pharmaceutically acceptable acid addition salt thereof. The novel caprazol derivatives now synthesized exhibit excellent antibacterial activities against a variety of bacteria including acid-fast bacteria.
摘要:
A caprazene-1"'-amide derivative and its 5"-N-alkoxycarbonyl or aralkyloxycarbonyl derivative which are represented by the following general formula (II)
wherein Me is methyl group, R 1 is a straight chain or a substantially straight chain alkyl group of 5-21 carbon atoms, a straight chain or a substantially straight chain alkenyl group of 5-21 carbon atoms or a cycloalkyl group of 5-12 carbon atoms, or R 1 is a phenyl group having a straight chain alkyl group of 1-14 carbon atoms or a straight chain alkoxy group of 1-9 carbon atoms or a cycloalkyl group of 5-12 carbon atoms at the para-position of the phenyl group, A is hydrogen atom or A is an amino-protecting group including an alkoxycarbonyl group, particularly tert-butoxycarbonyl group, or an aralkyloxycarbonyl group, particularly benzyloxycarbonyl group, or a pharmaceutically acceptable acid addition salt thereof
摘要:
A new compound, 3'-fluoro-3'-deoxykanamycin A is now provided, which is active against gram-negative and gram-positive bacteria, including kanamycin-resistant strains of bacteria and is useful as antibacterial agent for therapeutic treatment of bacterial infections. This new compound is produced by a process comprising reacting a 6- azido-2,4-di-O-protected-3,6-dideoxy-3-fluoro-α-D-glucopyranosyl bromide with the 4-hydroxyl group of a 6-0-(2'-0- protected-3'-N-protected-3'-amino-4',6'-di-O-protected-3'-deoxy-a-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the azido group of the resulting reaction product into an amino group, and removing the remaining protective groups from the reduction product.
摘要:
New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(a-hydroxy-w-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryt)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as anti-bacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-0-protected-2,3-6-trideoxy-2-fluoro-a-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-0-(2',4',6'-tri-0- protected-3'-N-protected-3'-amino-3'-deoxy-α-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.