The Nitrofuran-Warhead-Equipped Spirocyclic Azetidines Show Excellent Activity against <i>Mycobacterium tuberculosis</i>
Kristina Komarova,
Lyubov Vinogradova,
Alexey Lukin,
Maxim Zhuravlev,
Dmitry Deniskin,
Mikhail Chudinov,
Maxim Gureev,
Marine Dogonadze,
Natalia Zabolotnykh,
Tatiana Vinogradova,
Anastasia Lavrova,
Petr Yablonskiy
Affiliations
Kristina Komarova
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Lyubov Vinogradova
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Alexey Lukin
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Maxim Zhuravlev
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Dmitry Deniskin
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Mikhail Chudinov
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Maxim Gureev
Institute of Cytology, Russian Academy of Sciences, Tikhoretsky Ave 4, 194064 Saint Petersburg, Russia
Marine Dogonadze
Saint-Petersburg State Research Institute of Phthisiopulmonology of the Ministry of Healthcare of the Russian Federation, 191036 Saint Petersburg, Russia
Natalia Zabolotnykh
Saint-Petersburg State Research Institute of Phthisiopulmonology of the Ministry of Healthcare of the Russian Federation, 191036 Saint Petersburg, Russia
Tatiana Vinogradova
Saint-Petersburg State Research Institute of Phthisiopulmonology of the Ministry of Healthcare of the Russian Federation, 191036 Saint Petersburg, Russia
Anastasia Lavrova
Saint-Petersburg State Research Institute of Phthisiopulmonology of the Ministry of Healthcare of the Russian Federation, 191036 Saint Petersburg, Russia
Petr Yablonskiy
Department of Hospital Surgery, Faculty of Medicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia
A series of 21 new 7′H-spiro[azetidine-3,5′-furo [3,4-d]pyrimidine]s substituted at the pyrimidine ring second position were synthesized. The compounds showed high antibacterial in vitro activity against M. tuberculosis. Two compounds had lower minimum inhibitory concentrations against Mtb (H37Rv strain) compared with isoniazid. The novel spirocyclic scaffold shows excellent properties for anti-tuberculosis drug development.
