FARBER, Boris Slavinovich;ФАРБЕР, Борис Славинович;FARBER, Sof'ya Borisovna; Boris Slavinovich;ФАРБЕР, Софья Борисовна;FARBER
发明人:
MARTYNOV, Artur Viktorovich,МАРТЫНОВ, Артур Викторович
申请号：
RURU2017/000424
公开号：
WO2018/231091A1
申请日:
2017.06.16
申请国别(地区):
RU
年份:
2018
代理人:
摘要：
Field of use: the invention relates to combinatorial chemistry, pharmaceutics and cosmetology, and allows the synthesis of novel combinatorial libraries of antibiotic derivatives for use in pharmaceutics and cosmetology. Essence of the invention: novel combinatorial antibiotic derivatives based on supramolecular structures, characterized in that supramolecular structures (B) are produced by combinatorial synthesis from a single parent molecule of a polyfunctional antibiotic (A1) having two or more groups accessible for covalent modification in a reaction with at least two different modifiers (M2 and M3) simultaneously according to the synthesis scheme m А1+k М2 + k М3=m В, wherein a combinatorial mixture of modified derivatives of the parent molecule is formed having the greatest possible variety of derivatives, and as biologically active substances for creating pharmaceutical compositions, an entire combinatorial mixture is used in the form of a supramolecular structure without being split into individual components, and, in the reaction, a combinatorial mixture B of modified derivatives of the parent molecule of the antibiotic (A1) is formed which has a maximal (m) number of combinations. Technical result: modified combinatorial antibiotic derivatives having antimicrobial and antifungal activity toward multi-resistant and polyresistant strains of microorganisms and fungi. These agents have a broad spectrum of activity, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives prevent microorganisms from becoming habituated.La présente invention se rapporte au domaine de la chimie combinatoire, de la pharmacie et de la cosmétologie, et permet de synthétiser de nouvelles banques combinatoires de dérivés d'antibiotiques utilisés en pharmacie, en cosmétologie et en pharmacie. L'invention concerne essentiellement de nouveaux dérivés combinatoires d'antibiotiques à base de structures supramoléculaires, qui se caractérisent en ce que le
