Syntheses and antimicrobial activities of 9-O-acyl derivatives of tylosin and demycarosyltylosin.
نویسندگان
چکیده
منابع مشابه
Chemical modification of tylosin: synthesis of amino derivatives at C-20 position of tylosin and demycarosyltylosin.
Reductive aminations of the aldehyde group at C-20 position of tylosin and demycarosyltylosin (desmycosin) were carried out using primary and secondary amines in the presence of sodium cyanoborohydride. Some of these derivatives brought about higher antimicrobial and ribosome-binding activities, and the structure-activity relationship is discussed.
متن کاملChemical modification of tylosin. Thioether derivatives of tylosin and demycarosyltylosin.
Thioether derivatives of tylosin and demycarosyltylosin were synthesized by Michael-type addition of thiol to C-11 of the enone moiety on the aglycone. Some of tylosin derivatives were effective to macrolide resistant Staphylococcus aureus, and their in vivo activities were same or superior than that of tylosin.
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Essential roles for both the 23-O-mycinosyl and 4''-O-acyl moieties of 4''-O-acyltylosin derivatives in the expression of antimicrobial activity against multiple macrolide-resistant strains of Staphylococci and mycoplasmas were demonstrated by in vitro comparison of the MICs of erythromycin, josamycin, tylosin and its 3- and 4''-O-acyl derivatives, demycinosyltylosin (DMT) and its 3- and 4''-O-...
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The reaction of readily available 1 -methyl-4-nitropyrrole-2- carboxylic acid (1) with thionyl chloride afforded the corresponding acyl chloride 2. The reaction of compound 2 with thiosemicarbazides yielded 1-(1 -methyl-4-nitrop yrrole-2-carbony1)- thiosemicarbazides (3) which cyclized in basic medium to 5-(1-methyl-4-nitropyrrole- 2-y1)-2,4-dihydro-3H- l,2,4-triazole-3- thione 4. Alkylatio...
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A series of 2-(4-nitro-1-imidazolylmethyl)-1,3,4-oxadiazole, 1,3,4-triazole and 3-(4-nitro-1-imidazolylmethyl)-1,2,4-triazole derivatives were synthesized and tested for their antimicrobial activity. Some of the tested compounds were active against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Clostridium difficile, Aspergillus niger and Cryptococcus neoformans.
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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 39 12 شماره
صفحات -
تاریخ انتشار 1986