摘要:
Described is a method for the preparation of 6'-modified fortimicin compounds including 6'-epi fortimicin by converting 1,2-di-N-protected fortimicin B into 4,6'-di-N-substituted alkoxycarbonyl-1,2'-di-N-protected fortimicin B which is further converted to 1,2'-di-substituted fortimicin B-4,5-carbamate, a compound whose substitution pattern is particularly suited to modification at the 6'-amino group and novel compounds thereof.
摘要:
What is described is 2-epi-fortimicin A, 2-epi-fortimicin B or a 2-epi-fortimicin B derivative represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen or hydroxy; R.sub.3 is methyl or hydrogen; and R.sub.4 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoalkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, acyl of the formula ##STR2## wherein R.sub.5 is loweralkyl, aminoacyl, diaminoacyl, hydroxyacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue other than those defined above and the pharmaceutically acceptable salts thereof useful in the treatment of infections.
摘要:
2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
摘要:
A 1,2-modified fortimicin A or B represented by the formulae I, II and III: ##STR1## wherein R is hydrogen or loweralkyl; and R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-lower-alkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, amino hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N-N-diloweralkylaminohydroxyloweralkyl, acyl, aminoacyl, hydroxy-substituted aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N, N-diloweralkylaminoacyl, hydroxysubstituted-N-loweralkylaminoacyl and hydroxy-substituted-N, N-diloweralkylaminoacyl, and the pharmaceutically acceptable salts thereof. The compounds are broad spectrum antibiotics.
摘要:
2'-N-Acyl and alkyl fortimicin B and fortimicin B derivatives, 4,2'-N,N'-diacyl and dialkyl derivatives, 4-N-acyl-2'-N-alkyl and 4-N-alkyl-2'-N-acyl fortimicin B derivatives represented by the formula ##STR1## wherein: R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, hydroxyacyl, an amino acid residue, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl or N,N-diloweralkylaminohydroxyloweralkyl; and R.sub.1 is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl or hydrogen and the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are useful as antibiotics, intermediates, and are further useful in making moth proofing agents and pickling inhibitors.
摘要:
This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof.The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.
摘要:
2-Deoxyfortimicin, A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
摘要:
2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxysubstituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
摘要:
A 1,2-carbamate of fortimicin B and derivatives represented by the formula: ##STR1## wherein: R is hydrogen or monocyclicaryloxycarbonyl, R.sub.1 is hydrogen or monocyclicaryloxycarbonyl; and R.sub.2 is selected from the group consisting of loweralkyl, loweralkoxycarbonyl aminoloweralkyl, hydroxyloweralkyl, hydroxy-substituted aminolowerakyl, an amino acid residue, and N-protected amino acid residue, or when R and R.sub.1 are hydrogen, R.sub.2 can also be hydrogen; and the acid addition salts thereof when R,R.sub.1 or R.sub.2 are hydrogen or an unprotected aminoacid residue.
摘要:
An improved method for producing the antibiotic 2-deoxyfortimicin A, the method comprising the process of producing said antibiotic directly from fortimicin A in a four step process which results in a 50-60 percent yield of product.