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

22 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 - https://www.scopus.com/pages/publications/0037294166

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

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

M3 - Article

C2 - 12639539

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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