Biselyngbyaside, an 18-membered macrolide glycoside from marine cyanobacteria, and its derivatives are known to be sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) inhibitors. Recently, a SERCA orthologue of the malaria parasite, PfATP6, has attracted attention as a malarial drug target. To provide a novel drug lead, we designed new synthetic analogs of biselyngbyolide B, the aglycone of biselyngbyaside, based on the co-crystal structure of SERCA with biselyngbyolide B, and synthesized them using the established synthetic route for biselyngbyolide B. Their biological activities against malarial parasites were evaluated.

中文翻译：

---

海洋蓝细菌的Ca ²⁺泵抑制剂比塞林比德利德B的合成类似物的设计，合成和抗疟疾活性

Biselyngbyaside（一种来自海洋蓝细菌的18元大环内酯苷）及其衍生物是sarco /内质网Ca ²⁺ ATPase（SERCA）抑制剂。最近，作为疟疾药物的靶标，疟原虫的SERCA直系同源物PfATP6引起了人们的注意。为了提供新的药物线索，我们基于SERCA与比塞林比得利B的共晶体结构，设计了比塞林比得利B的糖苷配基的比塞林比得利B的新合成类似物，并使用确定的比塞林比得利B的合成路线合成了它们。对疟疾寄生虫进行了评估。