Dollinger L M, Howell A R
Department of Chemistry, University of Connecticut, Storrs 06269-4060, USA.
Bioorg Med Chem Lett. 1998 Apr 21;8(8):977-8. doi: 10.1016/s0960-894x(98)00140-1.
The 2-methyleneoxetane analog 2 of orlistat (OLS, 1) has been synthesized and tested against porcine pancreatic lipase (PPL). Despite the loss of the carbonyl group, a potential site for hydrogen bonding interaction with the enzyme and the key element in the acylation by OLS, 2 has activity comparable to 1.
奥利司他(OLS,1)的2-亚甲基氧杂环丁烷类似物2已被合成,并针对猪胰脂肪酶(PPL)进行了测试。尽管失去了羰基,这是与酶形成氢键相互作用的潜在位点以及OLS酰化作用中的关键元素,但2的活性与1相当。