Synthesis of Novel 1-Oxo-2,3,4-trisubstituted Tetrahydroisoquinoline Derivatives, Bearing Other Heterocyclic Moieties and Comparative Preliminary Study of Anti-Coronavirus Activity of Selected Compounds
Meglena I. Kandinska,
Nikola T. Burdzhiev,
Diana V. Cheshmedzhieva,
Sonia V. Ilieva,
Peter P. Grozdanov,
Neli Vilhelmova-Ilieva,
Nadya Nikolova,
Vesela V. Lozanova,
Ivanka Nikolova
Affiliations
Meglena I. Kandinska
Faculty of Chemistry and Pharmacy, University of Sofia St. Kliment Ohridski, 1 J. Bourchier Avenue, 1164 Sofia, Bulgaria
Nikola T. Burdzhiev
Faculty of Chemistry and Pharmacy, University of Sofia St. Kliment Ohridski, 1 J. Bourchier Avenue, 1164 Sofia, Bulgaria
Diana V. Cheshmedzhieva
Faculty of Chemistry and Pharmacy, University of Sofia St. Kliment Ohridski, 1 J. Bourchier Avenue, 1164 Sofia, Bulgaria
Sonia V. Ilieva
Faculty of Chemistry and Pharmacy, University of Sofia St. Kliment Ohridski, 1 J. Bourchier Avenue, 1164 Sofia, Bulgaria
Peter P. Grozdanov
Bulgarian Academy of Sciences, The Stephan Angeloff Institute of Microbiology, 26 Georgi Bonchev Street, 1113 Sofia, Bulgaria
Neli Vilhelmova-Ilieva
Bulgarian Academy of Sciences, The Stephan Angeloff Institute of Microbiology, 26 Georgi Bonchev Street, 1113 Sofia, Bulgaria
Nadya Nikolova
Bulgarian Academy of Sciences, The Stephan Angeloff Institute of Microbiology, 26 Georgi Bonchev Street, 1113 Sofia, Bulgaria
Vesela V. Lozanova
Department of Medical Chemistry and Biochemistry, Medical Faculty, Medical University-Sofia, 2 Zdrave Street, 1431 Sofia, Bulgaria
Ivanka Nikolova
Bulgarian Academy of Sciences, The Stephan Angeloff Institute of Microbiology, 26 Georgi Bonchev Street, 1113 Sofia, Bulgaria
A series of novel 1-oxo-2,3,4-trisubstituted tetrahydroisoquinoline (THIQ) derivatives bearing other heterocyclic moieties in their structure were synthesized based on the reaction between homophthalic anhydride and imines. Initial studies were carried out to establish the anti-coronavirus activity of some of the newly obtained THIQ-derivatives against two strains of human coronavirus-229E and OC-43. Their antiviral activity was compared with that of their close analogues, piperidinones and thiomorpholinones, previously synthesized in our group, with aim to expand the range of the tested representative sample and to obtain valuable preliminary information about biological properties of a wider variety of compounds.
