503174-32-1Relevant articles and documents
Synthesis and cyclooxygenase (COX-1/COX-2) inhibiting property of 3,4-diarylfuranones
Pal, Manojit,Veeramaneni, Venugopal Rao,Padakanti, Srinivas,Nagabelli, Murali,Vanguri, Akhila,Mamnoor, Premkumar,Casturi, Seshagiri Rao,Misra, Parimal,Mullangi, Ramesh,Yeleswarapu, Koteswar Rao
, p. 593 - 601 (2007/10/03)
A series of diarylfuranone including some 5-hydroxy derivatives and naphthofuranones have been synthesized as a unique class of COX-1/COX-2 inhibitors. In contrast to the earlier report of structurally similar rofecoxib, these compounds have been characterized as nonselective but highly potent COX inhibitors. Structure Activity Relationship study confirmed that methoxy and methylsulfanyl moieties are essential for COX activity and replacement or removal of any of this group affect COX-2 potency drastically rather than COX-1 efficacy. Studies on in vitro, in vivo screens and pharmacokinetics are discussed.