2. Academic Validation
  3. The Nitrofuran-Warhead-Equipped Spirocyclic Azetidines Show Excellent Activity against Mycobacterium tuberculosis

The Nitrofuran-Warhead-Equipped Spirocyclic Azetidines Show Excellent Activity against Mycobacterium tuberculosis

  • Molecules. 2024 Jun 27;29(13):3071. doi: 10.3390/molecules29133071.
Kristina Komarova 1,  Lyubov Vinogradova 1,  Alexey Lukin 1,  Maxim Zhuravlev 1,  Dmitry Deniskin 1,  Mikhail Chudinov 1,  Maxim Gureev 2,  Marine Dogonadze 3,  Natalia Zabolotnykh 3,  Tatiana Vinogradova 3,  Anastasia Lavrova 3 4,  Petr Yablonskiy 5
Affiliations

Affiliations

  • 1 Lomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119454 Moscow, Russia.
  • 2 Institute of Cytology, Russian Academy of Sciences, Tikhoretsky Ave 4, 194064 Saint Petersburg, Russia.
  • 3 Saint-Petersburg State Research Institute of Phthisiopulmonology of the Ministry of Healthcare of the Russian Federation, 191036 Saint Petersburg, Russia.
  • 4 Sophya Kovalevskaya North-West Mathematical Research Center, Immanuel Kant Baltic Federal University, 236041 Kaliningrad, Russia.
  • 5 Department of Hospital Surgery, Faculty of Medicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.
PMID: 38999023 DOI: 10.3390/molecules29133071
Abstract

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.

Keywords

antimycobacterial activity; deazaflavin-dependent nitroreductase; induced fit docking; nitrofurans; spiroazetidines; tuberculosis.

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