The Nitrofuran-Warhead-Equipped Spirocyclic Azetidines Show Excellent Activity against <i>Mycobacterium tuberculosis</i>

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

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