Chemistry Department, Emory University, Atlanta, GA 30322, USA.
ChemMedChem. 2021 Aug 19;16(16):2487-2490. doi: 10.1002/cmdc.202100134. Epub 2021 Apr 14.
3-Alkylpyridine alkaloids (3-APAs) isolated from the arctic sponge Haliclona viscosa are a promising group of bioactive marine alkaloids. However, due to limited bioavailability, investigations of their bioactivity have been hampered. Additionally, synthesis of a common intermediate requires the use of protecting groups and harsh conditions. In this work, we developed a simple and concise two-step route to nine different natural and synthetic haliclocyclins. These compounds displayed modest antibiotic activity against several Gram-positive bacterial strains.
从北极海绵 Haliclona viscosa 中分离得到的 3-烷基吡啶生物碱（3-APAs）是一组很有前途的海洋生物活性生物碱。然而，由于生物利用度有限，对其生物活性的研究受到了阻碍。此外，常见中间体的合成需要使用保护基团和苛刻的条件。在这项工作中，我们开发了一种简单明了的两步法合成九种不同的天然和合成的海鞘环素。这些化合物对几种革兰氏阳性菌表现出适度的抗生素活性。
