化学
甾醇O-酰基转移酶
取代基
结构-活动关系
选择性
同工酶
立体化学
转移酶
化学合成
酶
体外
生物化学
酶抑制剂
胆固醇
脂蛋白
催化作用
作者
Masaki Ohtawa,Hiroyuki Yamazaki,Satoshi Ohte,Daisuke Matsuda,Taichi Ohshiro,Lawrence L. Rudel,Satoshi Ōmura,Hiroshi Tomoda,Tohru Nagamitsu
标识
DOI:10.1016/j.bmcl.2012.12.099
摘要
In an effort to develop potent and selective inhibitors toward ACAT2, structure-activity relationship studies were carried out using derivatives based on pyripyropene A (PPPA, 1). We have successfully developed novel PPPA derivatives with a 7-O-substituted benzoyl substituent that significantly exhibit more potent ACAT2 inhibitory activity and higher ACAT2 isozyme selectivity than 1.
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