Alexander A. Kirichok, Hennadii Tkachuk, Kostiantyn Levchenko, Dmitry Granat, Tetyana Yegorova, Dmytro Lesyk, Anna Anisiforova, Yuliia Holota, Viktoriia Zomchak, Iryna Bodenchuk, Viktoriia Kosach, Petro Borysko, Rodion A. Korzh, Galeb Al-Maali, Vladimir Kubyshkin, Henry S. Rzepa, Pavel K. Mykhailiuk
{"title":"“Angular” Spirocyclic Azetidines: Synthesis, Characterization, and Evaluation in Drug Discovery","authors":"Alexander A. Kirichok, Hennadii Tkachuk, Kostiantyn Levchenko, Dmitry Granat, Tetyana Yegorova, Dmytro Lesyk, Anna Anisiforova, Yuliia Holota, Viktoriia Zomchak, Iryna Bodenchuk, Viktoriia Kosach, Petro Borysko, Rodion A. Korzh, Galeb Al-Maali, Vladimir Kubyshkin, Henry S. Rzepa, Pavel K. Mykhailiuk","doi":"10.1002/anie.202418850","DOIUrl":null,"url":null,"abstract":"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.","PeriodicalId":125,"journal":{"name":"Angewandte Chemie International Edition","volume":"18 1","pages":""},"PeriodicalIF":16.1000,"publicationDate":"2024-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Angewandte Chemie International Edition","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1002/anie.202418850","RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
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.
期刊介绍:
Angewandte Chemie, a journal of the German Chemical Society (GDCh), maintains a leading position among scholarly journals in general chemistry with an impressive Impact Factor of 16.6 (2022 Journal Citation Reports, Clarivate, 2023). Published weekly in a reader-friendly format, it features new articles almost every day. Established in 1887, Angewandte Chemie is a prominent chemistry journal, offering a dynamic blend of Review-type articles, Highlights, Communications, and Research Articles on a weekly basis, making it unique in the field.