NEW ANTIMICROBIAL AGENTS IN THE DIHYDROXANTHONE SERIES: ESTABLISHMENT OF STRUCTURE-ACTIVITY RELATIONSHIPS AND STANDARDIZATION

• DOI: 10.29296/25877313-2024-04-04
• Publication Date: 2024-07-14T21:09:21Z
• Authors: V.V. Frolova; N.A. Krishtanova; N.M. Chernov; S.V. Gurina; I.P. Yakovlev

Introduction. Irrational use of antimicrobial drugs, chemical and biological agents leads to the emergence spread resistance in microorgan-isms. Therefore, there is an increasing need for search development new compounds. Dihydroxanthone derivatives, which have a wide spectrum action, are one promising groups substances. New derivatives 4,4a-dihydroxanthone were obtained at St. Petersburg State Chemical Pharmaceutical University (SPCFU) Department Organic Chemistry. Synthetic 4,4a-dihydroxanthones structurally similar xanthones natural origin – fomalevones A C. compounds creation Purpose study. To establish relationship between structure synthesized dihydroxanthones their ac-tivity standardize active compound. Materials methods. 20 synthesized. The identity was estab-lished using physical methods analysis. activity these studied by double serial dilution method. Quality standards most compound 5-bromo-7-chloro-4,4-dimethyl-9-oxo-4,4a-dihydroxanthone (a17) developed. Results. In preliminary studies, we found that SPCFU pronounced effect against gram-positive bacteria. It found, antibacterial depended on structure. presence substituents with acceptor properties led increase activity, while donor reduced 5-Bromo-7-chloro-4,4-dimethyl-9-oxo-4,4a-dihydroxanthone turned out be compound, carried its standardization some indicators. Conclusions. During study dihydroxanthones, it they depends Among them, identified leader a17, has antistaphylococcal effect. Its been