Angew Chem Int Ed Engl 2024, e202418850
DOI: 10.1002/anie.202418850
Kirichok A. A.; Tkachuk H.; Levchenko K.; Granat D.; Yegorova T.; Lesyk D.; Anisiforova A.; Holota Y.; Zomchak V.; Bodenchuk I.; Kosach V.; Borysko P.; Korzh R. A.; Al-Maali G.; Kubyshkin V.; Rzepa H. S.; Mykhailiuk P. K.
The previously neglected “angular” spirocyclic azetidines have been synthesized, characterized, and validated in drug discovery. We have shown that these compounds could act as bioisosteres for common saturated six-membered heterocycles. Their incorporation into the structure of the anticancer drug Sonidegib (instead of morpholine), and Danofloxacine (instead of piperazine) provided novel patent-free analogs with similar physicochemical properties and high activity.