1-Azaspiro[3.3]heptane as a Bioisostere of Piperidine**,Angewandte Chemie International Edition

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1-Azaspiro[3.3]heptane as a Bioisostere of Piperidine**
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2023-10-11 , DOI: 10.1002/anie.202311583
Alexander A Kirichok _{1,

2} , Hennadii Tkachuk ₁ , Yevhenii Kozyriev _{1,

3} , Oleh Shablykin _{1,

4} , Oleksandr Datsenko ₁ , Dmitry Granat ₁ , Tetyana Yegorova ₂ , Yuliya P Bas ₂ , Vitalii Semirenko ₁ , Iryna Pishel ₁ , Vladimir Kubyshkin ₁ , Dmytro Lesyk ₅ , Oleksii Klymenko-Ulianov ₅ , Pavel K Mykhailiuk _{1,

2}

Affiliation

1-Azaspiro[3.3]heptanes were synthesized, characterized, and validated biologically as bioisosteres of piperidine. Incorporation of this core into the anesthetic drug bupivacaine instead of the piperidine ring resulted in a patent-free analogue with high activity.

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