Discovery of Potent Benzoselenazinone-Based DprE1 Inhibitors: A Novel Selenium-Containing Scaffold with Superior Anti-TB Activity and Pharmacokinetic Properties
of BTZs in CD-1 mice, positioning it as a promising preclinical candidate. This study highlights the potential of selenium-based bioisosteres in anti-TB drug discovery and offers a novel benzoselenazinone scaffold with enhanced efficacy and safety for further development.
Authors
- Andrea Tresoldi (ORCID: https://orcid.org/0009-0005-7190-380X)
- H Huang
- Matteo Mori (ORCID: https://orcid.org/0000-0002-7491-1494)
- Mario Cocorullo (ORCID: https://orcid.org/0000-0001-7074-0328)
- Bo Wang (ORCID: https://orcid.org/0000-0001-5132-7685)
- Laurent Robert Chiarelli (ORCID: https://orcid.org/0000-0003-0348-9764)
- Peng Li (ORCID: https://orcid.org/0000-0003-1626-3385)
- Yu Lu (ORCID: https://orcid.org/0009-0004-8398-1592)
- Chengxia Mao
- Yang Liu
- Xiuli Xu
Institutions
- Chinese Center For Disease Control and Prevention (CN)
- University of Milan (IT)
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- National Medical Products Administration (CN)
- University of Pavia (IT)
- Beijing Chest Hospital (CN)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-04-17
- DOI
- https://doi.org/10.1021/acs.jmedchem.5c03770
- Primary Topic
- Organoselenium and organotellurium chemistry
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Chinese Academy of Medical Sciences
- Beijing Municipal Natural Science Foundation