Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor

Hyeung Geun Park; Mi Kyung Park; Ji Yeon Choi; Sea Hoon Choi; Jihye Lee; Boon Saeng Park; Myoung Goo Kim; Young Ger Suh; Hawon Cho; Uhtaek Oh; Jeewoo Lee; Hee Doo Kim; Young Ho Park; Hyun Ju Koh; Kyung Min Lim; Joo Hyun Moh; Sang Sup Jew

doi:10.1016/S0960-894X(02)01040-5

Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor

Hyeung Geun Park, Mi Kyung Park, Ji Yeon Choi, Sea Hoon Choi, Jihye Lee, Boon Saeng Park, Myoung Goo Kim, Young Ger Suh, Hawon Cho, Uhtaek Oh, Jeewoo Lee, Hee Doo Kim, Young Ho Park, Hyun Ju Koh, Kyung Min Lim, Joo Hyun Moh, Sang Sup Jew

Department of Pharmaceutical Sciences

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

21 Scopus citations

Abstract

Twenty-seven N,N′,N″-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4′-hydroxy-3′-methoxy-phenyl)-propyl]-1,3-diphenethyl- thiourea (8l, IC₅₀=0.32 μM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC₅₀=0.65 μM) against the vanilloid receptor in a ⁴⁵Ca²⁺-influx assay.

Original language	English
Pages (from-to)	601-604
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	4
DOIs	https://doi.org/10.1016/S0960-894X(02)01040-5
State	Published - Feb 2003

Bibliographical note

Funding Information:
This research was supported by a grant from Amore Pacific Co. Ltd., Korea, and a grant of the Korea Health 21 R&D Project, Ministry of Health & Welfare, Republic of Korea: 02-PJ2-PG4-PT01-0014.

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Park, H. G., Park, M. K., Choi, J. Y., Choi, S. H., Lee, J., Park, B. S., Kim, M. G., Suh, Y. G., Cho, H., Oh, U., Lee, J., Kim, H. D., Park, Y. H., Koh, H. J., Lim, K. M., Moh, J. H., & Jew, S. S. (2003). Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor. Bioorganic and Medicinal Chemistry Letters, 13(4), 601-604. https://doi.org/10.1016/S0960-894X(02)01040-5

@article{3729f68a4fff4bbc8490c12847b27db5,

title = "Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor",

abstract = "Twenty-seven N,N′,N″-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4′-hydroxy-3′-methoxy-phenyl)-propyl]-1,3-diphenethyl- thiourea (8l, IC50=0.32 μM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC50=0.65 μM) against the vanilloid receptor in a 45Ca2+-influx assay.",

author = "Park, {Hyeung Geun} and Park, {Mi Kyung} and Choi, {Ji Yeon} and Choi, {Sea Hoon} and Jihye Lee and Park, {Boon Saeng} and Kim, {Myoung Goo} and Suh, {Young Ger} and Hawon Cho and Uhtaek Oh and Jeewoo Lee and Kim, {Hee Doo} and Park, {Young Ho} and Koh, {Hyun Ju} and Lim, {Kyung Min} and Moh, {Joo Hyun} and Jew, {Sang Sup}",

note = "Funding Information: This research was supported by a grant from Amore Pacific Co. Ltd., Korea, and a grant of the Korea Health 21 R&D Project, Ministry of Health & Welfare, Republic of Korea: 02-PJ2-PG4-PT01-0014.",

year = "2003",

month = feb,

doi = "10.1016/S0960-894X(02)01040-5",

language = "English",

volume = "13",

pages = "601--604",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "4",

}

Park, HG, Park, MK, Choi, JY, Choi, SH, Lee, J, Park, BS, Kim, MG, Suh, YG, Cho, H, Oh, U, Lee, J, Kim, HD, Park, YH, Koh, HJ, Lim, KM, Moh, JH & Jew, SS 2003, 'Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor', Bioorganic and Medicinal Chemistry Letters, vol. 13, no. 4, pp. 601-604. https://doi.org/10.1016/S0960-894X(02)01040-5

TY - JOUR

T1 - Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor

AU - Park, Hyeung Geun

AU - Park, Mi Kyung

AU - Choi, Ji Yeon

AU - Choi, Sea Hoon

AU - Lee, Jihye

AU - Park, Boon Saeng

AU - Kim, Myoung Goo

AU - Suh, Young Ger

AU - Cho, Hawon

AU - Oh, Uhtaek

AU - Lee, Jeewoo

AU - Kim, Hee Doo

AU - Park, Young Ho

AU - Koh, Hyun Ju

AU - Lim, Kyung Min

AU - Moh, Joo Hyun

AU - Jew, Sang Sup

N1 - Funding Information: This research was supported by a grant from Amore Pacific Co. Ltd., Korea, and a grant of the Korea Health 21 R&D Project, Ministry of Health & Welfare, Republic of Korea: 02-PJ2-PG4-PT01-0014.

PY - 2003/2

Y1 - 2003/2

N2 - Twenty-seven N,N′,N″-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4′-hydroxy-3′-methoxy-phenyl)-propyl]-1,3-diphenethyl- thiourea (8l, IC50=0.32 μM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC50=0.65 μM) against the vanilloid receptor in a 45Ca2+-influx assay.

AB - Twenty-seven N,N′,N″-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4′-hydroxy-3′-methoxy-phenyl)-propyl]-1,3-diphenethyl- thiourea (8l, IC50=0.32 μM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC50=0.65 μM) against the vanilloid receptor in a 45Ca2+-influx assay.

UR - http://www.scopus.com/inward/record.url?scp=0037294166&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(02)01040-5

DO - 10.1016/S0960-894X(02)01040-5

M3 - Article

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AN - SCOPUS:0037294166

SN - 0960-894X

VL - 13

SP - 601

EP - 604

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor

Abstract

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