A prodrug approach to COX-2 inhibitors with methylsulfone

Joo Hyun Moh; Young Hoon Choi; Kyoung Min Lim; Ki Wha Lee; Song Seok Shin; Jin Kyu Choi; Hyun Joo Koh; Shin Chung

doi:10.1016/j.bmcl.2004.01.048

A prodrug approach to COX-2 inhibitors with methylsulfone

Joo Hyun Moh
, Young Hoon Choi
, Kyoung Min Lim
, Ki Wha Lee
, Song Seok Shin
, Jin Kyu Choi
, Hyun Joo Koh
, Shin Chung

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

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.

Original language	English
Pages (from-to)	1757-1760
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2004.01.048
State	Published - Apr 2004

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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.",

author = "Moh, \{Joo Hyun\} and Choi, \{Young Hoon\} and Lim, \{Kyoung Min\} and Lee, \{Ki Wha\} and Shin, \{Song Seok\} and Choi, \{Jin Kyu\} and Koh, \{Hyun Joo\} and Shin Chung",

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T1 - A prodrug approach to COX-2 inhibitors with methylsulfone

AU - Moh, Joo Hyun

AU - Choi, Young Hoon

AU - Lim, Kyoung Min

AU - Lee, Ki Wha

AU - Shin, Song Seok

AU - Choi, Jin Kyu

AU - Koh, Hyun Joo

AU - Chung, Shin

PY - 2004/4

Y1 - 2004/4

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/1542613874

U2 - 10.1016/j.bmcl.2004.01.048

DO - 10.1016/j.bmcl.2004.01.048

M3 - Article

C2 - 15026065

AN - SCOPUS:1542613874

SN - 0960-894X

VL - 14

SP - 1757

EP - 1760

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

A prodrug approach to COX-2 inhibitors with methylsulfone

Abstract

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