Appleton R A, Brown K
Prostaglandins. 1979 Jul;18(1):29-34. doi: 10.1016/s0090-6980(79)80020-9.
When space-filling models of the peroxy radical precursor of PGG were compared with models of 2(S)-(3-chloro-4-cyclohexylphenyl) propionic acid and other acidic cyclooxygenase inhibitors several common structural features were revealed. This led us to propose a template for designing non-steroidal anti-inflammatory drugs (NSAID's) based on the conformation of the peroxy radical immediately prior to its cyclisation to PGG. The template can be equated with a complementary cyclooxygenase receptor site.
当将PGG过氧自由基前体的空间填充模型与2(S)-(3-氯-4-环己基苯基)丙酸及其他酸性环氧化酶抑制剂的模型进行比较时,发现了几个共同的结构特征。这使我们基于过氧自由基环化形成PGG之前的构象,提出了一种设计非甾体抗炎药(NSAID)的模板。该模板可等同于一个互补的环氧化酶受体位点。