6-Arylamino-5,8-quinazolinediones as potent inhibitors of endothelium-dependent vasorelaxation

Chung Kyu Ryu; Keun Hwa Shin; Ji Hui Seo; Hwa Jung Kim

doi:10.1016/S0223-5234(01)01290-9

6-Arylamino-5,8-quinazolinediones as potent inhibitors of endothelium-dependent vasorelaxation

Chung Kyu Ryu, Keun Hwa Shin, Ji Hui Seo, Hwa Jung Kim

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

17 Scopus citations

Abstract

6-(Substituted-phenyl)amino-5,8-quinazolinediones (3) were synthesised by regioselective substitution of 5,8-quinazolinedione (5) with appropriate arylamines in the presence of Ce(III) ions. All synthesised 5,8-quinazolinediones 3 showed a potent and efficacious inhibitory effect on the acetylcholine (ACh)-induced vasorelaxation of rat aorta with the endothelium. The quinones 3, at a low concentration of 0.1 μM, reduced the maximal response with increase of EC₅₀ values for ACh. The results indicate that quinones 3 are potent inhibitors of endothelium-dependent vasorelaxation.

Original language	English
Pages (from-to)	77-82
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	37
Issue number	1
DOIs	https://doi.org/10.1016/S0223-5234(01)01290-9
State	Published - 1 Jan 2002

Keywords

6-arylamino-5,8-quinazolinedione
Endothelium-dependent vasorelaxation
Inhibitors
Isosteres

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10.1016/S0223-5234(01)01290-9

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title = "6-Arylamino-5,8-quinazolinediones as potent inhibitors of endothelium-dependent vasorelaxation",

abstract = "6-(Substituted-phenyl)amino-5,8-quinazolinediones (3) were synthesised by regioselective substitution of 5,8-quinazolinedione (5) with appropriate arylamines in the presence of Ce(III) ions. All synthesised 5,8-quinazolinediones 3 showed a potent and efficacious inhibitory effect on the acetylcholine (ACh)-induced vasorelaxation of rat aorta with the endothelium. The quinones 3, at a low concentration of 0.1 μM, reduced the maximal response with increase of EC50 values for ACh. The results indicate that quinones 3 are potent inhibitors of endothelium-dependent vasorelaxation.",

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author = "Ryu, \{Chung Kyu\} and Shin, \{Keun Hwa\} and Seo, \{Ji Hui\} and Kim, \{Hwa Jung\}",

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doi = "10.1016/S0223-5234(01)01290-9",

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TY - JOUR

T1 - 6-Arylamino-5,8-quinazolinediones as potent inhibitors of endothelium-dependent vasorelaxation

AU - Ryu, Chung Kyu

AU - Shin, Keun Hwa

AU - Seo, Ji Hui

AU - Kim, Hwa Jung

PY - 2002/1/1

Y1 - 2002/1/1

N2 - 6-(Substituted-phenyl)amino-5,8-quinazolinediones (3) were synthesised by regioselective substitution of 5,8-quinazolinedione (5) with appropriate arylamines in the presence of Ce(III) ions. All synthesised 5,8-quinazolinediones 3 showed a potent and efficacious inhibitory effect on the acetylcholine (ACh)-induced vasorelaxation of rat aorta with the endothelium. The quinones 3, at a low concentration of 0.1 μM, reduced the maximal response with increase of EC50 values for ACh. The results indicate that quinones 3 are potent inhibitors of endothelium-dependent vasorelaxation.

AB - 6-(Substituted-phenyl)amino-5,8-quinazolinediones (3) were synthesised by regioselective substitution of 5,8-quinazolinedione (5) with appropriate arylamines in the presence of Ce(III) ions. All synthesised 5,8-quinazolinediones 3 showed a potent and efficacious inhibitory effect on the acetylcholine (ACh)-induced vasorelaxation of rat aorta with the endothelium. The quinones 3, at a low concentration of 0.1 μM, reduced the maximal response with increase of EC50 values for ACh. The results indicate that quinones 3 are potent inhibitors of endothelium-dependent vasorelaxation.

KW - 6-arylamino-5,8-quinazolinedione

KW - Endothelium-dependent vasorelaxation

KW - Inhibitors

KW - Isosteres

UR - https://www.scopus.com/pages/publications/0036176128

U2 - 10.1016/S0223-5234(01)01290-9

DO - 10.1016/S0223-5234(01)01290-9

M3 - Article

C2 - 11841877

AN - SCOPUS:0036176128

SN - 0223-5234

VL - 37

SP - 77

EP - 82

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 1

ER -

6-Arylamino-5,8-quinazolinediones as potent inhibitors of endothelium-dependent vasorelaxation

Abstract

Keywords

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