Synthesis and Antimicrobial Activity of 2,5-Diaryl-8,8-Dimethyl-3,6,7,8-Tetrahydro-2H-Pyrido[4,3,2-de]Cinnolin-3-Ones

• Published in: Pharmaceutical chemistry journal 2023-08, Vol.57 (5), p.632-636
• Main Authors: Shurov, S. N., Lystsova, E. A., Zykova, S. S., Namyatova, K. V., Chernykh, T. F., Bogdanova, O. Yu, Tsvetkova, I. A.
• Format: Article
• Language: English
• Subjects: Antifungal agents; Bacteria; Medicine; Molds (Fungi); Organic Chemistry; Pharmacology/Toxicology; Pharmacy; Search for New Drugs
• ISSN: 0091-150X; 1573-9031
• DOI: 10.1007/s11094-023-02930-0

The computer program Prediction of Activity Spectra for Substances (PASS), which allows a prediction of the spectrum of biological activity of chemical compounds based on an analysis of their structure(activity relationships, was used to predict the biological activity of new promising derivatives of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2 H -pyrido[4,3,2- de ]cinnolin-3-ones. Screening of the compounds found that 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2 H -pyrido[4,3,2- de ]cinnolin-3-ones could exhibit antibacterial and antifungal activity. The antimicrobial activity of the synthesized compounds was studied against Gram-positive and Gram-negative bacteria and yeast and mold fungi. The compounds were shown to have an inhibitory effect on some types of Gram-positive bacteria and fungi. 8,8-Dimethyl-2- p -tolyl-5- p -chlorophenyl-3,7,8,9-tetrahydro-2 H -pyrido[4,3,2- de ]cinnolin-3-one had a minimum inhibitory concentration of 48 μg/mL for Gram-positive bacteria and possessed the most pronounced antimicrobial activity of the tested compounds.