Department of Medicinal Chemistry, University of Florida, Gainesville, Florida 32610, USA.
Org Lett. 2013 Aug 16;15(16):4050-3. doi: 10.1021/ol401396u. Epub 2013 Aug 5.
Novel bioactive lipids were identified from a Guamanian cyanobacterium, the Pseudomonas aeruginosa quorum sensing inhibitor pitinoic acid A (1) and the anti-inflammatory pitinoic acids B (2) and C. The structure of 2 was confirmed by synthesis, which also allowed for biological evaluation. Since 2 is an ester of pitinoic acids A and C, it represents a prodrug strategy to liberate dual biological activity for the management of P. aeruginosa infections and their associated inflammation.
从关岛的一种蓝细菌中鉴定出新型生物活性脂质,绿脓杆菌群体感应抑制剂派啶酸 A(1)和具有抗炎活性的派啶酸 B(2)和 C。通过合成确定了 2 的结构,这也允许进行生物学评价。由于 2 是派啶酸 A 和 C 的酯,因此它代表了一种前药策略,可以释放双重生物学活性,用于治疗铜绿假单胞菌感染及其相关炎症。