Kurniawan Yudhi Dwi, Tachrim Zetryana Puteri, Ernawati Teni, Hermawan Faris, Nurasiyah Ima, Sulmantara Muhammad Alfin
Research Center for Pharmaceutical Ingredient and Traditional Medicine, National Research and Innovation Agency (BRIN), Tangerang Selatan, Banten 15314, Indonesia.
Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Negeri Semarang, Semarang, Central Java 50229, Indonesia.
Beilstein J Org Chem. 2025 Jun 12;21:1135-1160. doi: 10.3762/bjoc.21.91. eCollection 2025.
Borrelidin, a naturally occurring antibiotic, has attracted considerable interest due to its diverse biological activities and complex molecular architecture. Although extensive research has explored its pharmacological properties and various synthetic approaches, significant challenges remain in the efficient synthesis of borrelidin and its analogs. Existing literature largely focuses on total synthesis, bioactivity, and structural modifications, leaving a notable gap in fragment-focused synthesis, particularly for its intricate substructures. This review seeks to address this gap by offering a detailed examination of borrelidin fragment synthesis, highlighting key challenges and innovative strategies involved. By pinpointing unresolved synthetic hurdles, this work advocates for a fragment-focused approach as a crucial step toward advancing borrelidin research and expanding its potential applications.
硼雷素是一种天然存在的抗生素,因其多样的生物活性和复杂的分子结构而备受关注。尽管已有广泛研究探索了其药理性质和各种合成方法,但在硼雷素及其类似物的高效合成方面仍存在重大挑战。现有文献主要集中在全合成、生物活性和结构修饰上,在以片段为重点的合成方面存在显著空白,尤其是对于其复杂的亚结构。本综述旨在通过详细考察硼雷素片段合成来填补这一空白,突出其中涉及的关键挑战和创新策略。通过明确未解决的合成障碍,这项工作倡导以片段为重点的方法,作为推进硼雷素研究和扩大其潜在应用的关键一步。