一种含甲基砜的COX-2抑制剂的前药方法。
A prodrug approach to COX-2 inhibitors with methylsulfone.
作者信息
Moh Joo Hyun, Choi Young Hoon, Lim Kyoung Min, Lee Ki-Wha, Shin Song Seok, Choi Jin Kyu, Koh Hyun Joo, Chung Shin
机构信息
Drug Discovery, AmorePacific R&D Center, 314-1 Bora-ri, Giheung-eup, Yongin, Gyeonggi-do 449-729, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1757-60. doi: 10.1016/j.bmcl.2004.01.048.
2,2-dimethyl-4-phenyl-5-[4-(methylsulfinyl)phenyl]-3(2H)furanone derivatives, 3 and 6, were shown to be effectively transformed in vivo into the corresponding methylsulfone derivatives 1 and 4, when orally administered to rats. Pharmacological implications for use of sulfoxide analogues 3 and 6 are discussed as prodrugs to potent selective COX-2 inhibitors 1 and 4.
2,2-二甲基-4-苯基-5-[4-(甲基亚磺酰基)苯基]-3(2H)呋喃酮衍生物3和6经对大鼠口服给药后，显示在体内可有效转化为相应的甲基砜衍生物1和4。文中讨论了将亚砜类似物3和6作为强效选择性COX-2抑制剂1和4的前药的药理学意义。
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