Chun-Lan Xie, Hong-Xiu Xiao, Pei-Fang Song, Qing-Mei Liu, Haoxiang Wei, Liang Wu, Guang-Hao Zhu, Guang-Ming Liu, Yandong Zhang, Ping Wang, Xian-Wen Yang
Food allergy (FA) poses a growing global food safety concern, yet no effective cure exists in clinics. Previously, we discovered a potent antifood allergy compound, butyrolactone I (BTL-I, 1 ), from the deep sea. Unfortunately, it has a very low exposure and poor pharmacokinetic (PK) profile in rats. Therefore, a series of structural optimizations toward the metabolic pathways of BTL-I were conducted to provide 18 derives ( 2 - 19 ). Among them, BTL-MK ( 19 ) showed superior antiallergic activity and favorable pharmacokinetics compared to BTL-I, being twice as potent with a clearance (CL) rate of only 0...
April 19, 2024: Journal of Medicinal Chemistry