title: A prodrug approach to COX-2 inhibitors with methylsulfone.
abstract: 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.
authors.affiliation: Drug Discovery, AmorePacific R&D Center, 314-1 Bora-ri, Giheung-eup, Yongin, Gyeonggi-do 449-729, Republic of Korea.
authors.forename: Joo Hyun
authors.initials: JH
authors.lastname: Moh
authors.forename: Young Hoon
authors.initials: YH
authors.lastname: Choi
authors.forename: Kyoung Min
authors.initials: KM
authors.lastname: Lim
authors.forename: Ki-Wha
authors.initials: KW
authors.lastname: Lee
authors.forename: Song Seok
authors.initials: SS
authors.lastname: Shin
authors.forename: Jin Kyu
authors.initials: JK
authors.lastname: Choi
authors.forename: Hyun Joo
authors.initials: HJ
authors.lastname: Koh
authors.forename: Shin
authors.initials: S
authors.lastname: Chung
mesh_terms: D000818:Animals; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry; D004121:Dimethyl Sulfoxide; D004305:Dose-Response Relationship, Drug; D008297:Male; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D011917:Rats, Inbred Lew; D017207:Rats, Sprague-Dawley; D013450:Sulfones / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D016861:Cyclooxygenase Inhibitors; D011355:Prodrugs; D013450:Sulfones; C025910:dimethyl sulfone; D004121:Dimethyl Sulfoxide