4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor

Ki Jun Hwang; Tae Suk Lee; Ki Won Kim; Beom Tae Kim; Chul Min Lee; Eun Young Park; Ran Sook Woo

doi:10.1007/BF02975090

4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor

Ki Jun Hwang^*
, Tae Suk Lee
, Ki Won Kim
, Beom Tae Kim
, Chul Min Lee
, Eun Young Park
, Ran Sook Woo

^*Corresponding author for this work

Department of Bioenvironmental Chemistry

Jeonbuk National University

Research output: Contribution to journal › Journal article › peer-review

7 Scopus citations

Abstract

Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (binding assay) for NMDA receptor glycine site.

Original language	English
Pages (from-to)	270-275
Number of pages	6
Journal	Archives of Pharmacal Research
Volume	24
Issue number	4
DOIs	https://doi.org/10.1007/BF02975090
State	Published - 2001.08

Keywords

4-Hydroxy quinolone
Bioisosteres
Glycine site
Nmda Receptor
Thieno[2,3-b] pyrimidine

Quacquarelli Symonds(QS) Subject Topics

Medicine
Engineering - Petroleum
Pharmacy & Pharmacology
Chemistry

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10.1007/BF02975090

Cite this

@article{09ead0e82c1b45f0859f9a22cf9cc8a6,

title = "4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor",

abstract = "Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (binding assay) for NMDA receptor glycine site.",

keywords = "4-Hydroxy quinolone, Bioisosteres, Glycine site, Nmda Receptor, Thieno[2,3-b] pyrimidine",

author = "Hwang, \{Ki Jun\} and Lee, \{Tae Suk\} and Kim, \{Ki Won\} and Kim, \{Beom Tae\} and Lee, \{Chul Min\} and Park, \{Eun Young\} and Woo, \{Ran Sook\}",

year = "2001",

month = aug,

doi = "10.1007/BF02975090",

language = "English",

volume = "24",

pages = "270--275",

journal = "Archives of Pharmacal Research",

issn = "0253-6269",

number = "4",

}

4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor. / Hwang, Ki Jun; Lee, Tae Suk; Kim, Ki Won et al.
In: Archives of Pharmacal Research, Vol. 24, No. 4, 08.2001, p. 270-275.

Research output: Contribution to journal › Journal article › peer-review

TY - JOUR

T1 - 4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives

T2 - Synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor

AU - Hwang, Ki Jun

AU - Lee, Tae Suk

AU - Kim, Ki Won

AU - Kim, Beom Tae

AU - Lee, Chul Min

AU - Park, Eun Young

AU - Woo, Ran Sook

PY - 2001/8

Y1 - 2001/8

N2 - Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (binding assay) for NMDA receptor glycine site.

AB - Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (binding assay) for NMDA receptor glycine site.

KW - 4-Hydroxy quinolone

KW - Bioisosteres

KW - Glycine site

KW - Nmda Receptor

KW - Thieno[2,3-b] pyrimidine

UR - https://www.scopus.com/pages/publications/0035430306

U2 - 10.1007/BF02975090

DO - 10.1007/BF02975090

M3 - Journal article

C2 - 11534755

AN - SCOPUS:0035430306

SN - 0253-6269

VL - 24

SP - 270

EP - 275

JO - Archives of Pharmacal Research

JF - Archives of Pharmacal Research

IS - 4

ER -

4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor

Abstract

Keywords

Quacquarelli Symonds(QS) Subject Topics

Access to Document

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