FIELD: pharmacology.
SUBSTANCE: invention relates to the field of synthesis of biologically active analogues of natural compounds, namely to the production of a new representative of acetylene derivatives of fusidic acid: prop-2-in-1-il-(2Z)-2-[(3α, 4α, 8α, 11α, 14β, 16β)-16-(acetyloxy)-3,11-dihydroxy-4,8,10,14-tetramethylgonane-17-ylidene]-6-methylhept-5-enoate, which has high antibacterial activity against Staphylococcus aureus (MRSA) with low toxicity, showing minimal hemolytic effect at the maximum tested concentration. Prop-2-in-1-il-(2Z)-2-[(3α, 4α, 8α, 11α, 14β, 16β)-16-( acetyloxy)-3.11-dihydroxy-4,8,10,14-tetramethylgonane-17-ylidene]-6-methylhept-5-enoate was obtained on the basis of fusidic acid by interaction with an equimolar amount of propargyl bromide in an acetone medium during boiling for 2 hours using K2CO3 as a base. The yield of prop-2-in-1-il-(2Ζ)-2-[(3α, 4α, 8α, 11α, 14β, 16β)-16-( acetyloxy)-3.11-dihydroxy-4,8,10,14-tetramethylgonane-17-ylidene]-6-methylhept-5-enoate was 99%.
EFFECT: expansion of the range of solutions to resist Staphylococcus aureus.
3 cl, 2 ex, 1 tbl
| Title |
Year |
Author |
Number |
| (2Z)-2-[(3Β, 4Α, 8Α, 11Α, 14Β, 16Β)-16-(ACETYLOXY)-3-({3-[(4-AMINOBUTYL)AMINO]PROPYL}AMINO)-11-HYDROXY-4,8,10,14-TETRAMETHYL GONANE-17-YLIDENE]-6-METHYLHEPT-5-ENOIC ACID WITH ANTIMICROBIAL AND FUNGICIDAL ACTIVITY AND METHOD FOR PRODUCTION THEREOF |
2019 |
- Salimova Elena Viktorovna
- Tretyakova Elena Valerevna
- Parfenova Lyudmila Vyacheslavovna
|
RU2730604C1 |
| N,N'-BIS(3-AMINOPROPYL)BUTANE-1,4-DIAMINO DERIVATIVES OF FUSIDIC ACID, HAVING A WIDE SPECTRUM OF ANTIMICROBIAL ACTIVITY |
2019 |
- Salimova Elena Viktorovna
- Tretyakova Elena Valerevna
- Parfenova Lyudmila Vyacheslavovna
|
RU2726196C1 |
| (2Z)-2-[(4Α, 5Α, 8Α, 9Β, 13Α, 14Β, 16Β)-16-(ACETYLOXY)-3(Z),11(E)-BIS (HYDROXYIMINO)-4,8,10,14-TETRAMETHYLGONANE-17-YLIDENE]-6-METHYLHEPT-5-ENOIC ACID, METHOD OF PRODUCING AND ANTIMICROBIAL PROPERTIES |
2019 |
- Salimova Elena Viktorovna
- Tretyakova Elena Valerevna
- Parfenova Lyudmila Vyacheslavovna
|
RU2726122C1 |
| NEW AMINE DERIVATIVES OF FUSIDIC ACID EXHIBITING ANTITUMOUR ACTIVITY |
2019 |
- Salimova Elena Viktorovna
- Tretyakova Elena Valerevna
- Parfenova Lyudmila Vyacheslavovna
|
RU2735665C1 |
| NEW NAPHTHO[2,1-B]CARBAZOL DERIVATIVES OF FUSIDIC ACID, METHOD OF SYNTHESIS AND ANTI-MICROBIAL PROPERTIES |
2019 |
- Salimova Elena Viktorovna
- Tretyakova Elena Valerevna
- Parfenova Lyudmila Vyacheslavovna
- Dzhemilev Usein Memetovich
|
RU2746947C2 |
| (1-BENZYL-1H-1,2,3-TRIAZOL-4-YL)METHYL (Z)-2-((3S,4S,8S,10S,11R,14S,16S)-16-ACETOXY-3,11 -DIHYDROXY-4,8,10,14-TETRAMETHYLHEXADECAHYDRO-17H-CYCLOPENTA[a]PHENANTHRENE-17-YLIDENE)-6-METHYLHEPT-5-ENOATE EXHIBITING ANTIBACTERIAL AND FUNGICIDAL ACTIVITY |
2022 |
- Salimova Elena Viktorovna
- Parfenova Liudmila Viacheslavovna
|
RU2784215C1 |
| USE OF MANNICH BASES BASED ON FUSIDIC ACID AS COMPOUNDS WITH ANTI-TUMOUR ACTIVITY |
2023 |
- Salimova Elena Viktorovna
- Parfenova Liudmila Viacheslavovna
- Ishmetova Diana Valievna
- Zainullina Liana Fanzilevna
- Vakhitova Iuliia Venerovna
|
RU2819293C1 |
| DERIVATIVE OF FUSIDIC ACID, STEREOISOMER, PHARMACEUTICAL COMPOSITIONS, COMPOUNDS |
2000 |
- Duvoll' Ture
- Fon Dene Vel'F
|
RU2257391C2 |
| COMBINATIONS OF ALPHA-2-DELTA-LIGAND WITH SELECTIVE CYCLOIXYGENASE-2 INHIBITOR |
2003 |
- Tehjlor Charl'Z Prajs Ml.
|
RU2286151C2 |
| USE OF SILVER SALTS OF METHYL (2Z)-4-ARYL-2-{4-[(4,6-DIMETHYLPYRIMIDIN-2-YL)SULFAMOYL]PHENYLAMINO}-4-OXOBUT-2-ENOATES AS ANTIBACTERIAL AGENTS |
2022 |
- Gein Vladimir Leonidovich
- Bobrovskaia Olga Vasilevna
- Novikova Valentina Vasilevna
- Makhmudov Ramiz Ragibovich
- Mashkina Elena Aleksandrovna
|
RU2793327C1 |
