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

10 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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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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