Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists

A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. ( R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed th...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-04, Vol.14 (7), p.1751-1755
Hauptverfasser:	Ryu, Chong Hyun, Jang, Mi Jung, Jung, Jeong Wha, Park, Ju-Hyun, Choi, Hye Young, Suh, Young-ger, Oh, Uhtaek, Park, Hyeung-geun, Lee, Jeewoo, Koh, Hyun-Joo, Mo, Joo-Hyun, Joo, Yung Hyup, Park, Young-Ho, Kim, Hee-Doo
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics Animals Biological and medical sciences Cells, Cultured Medical sciences Neurons, Afferent - drug effects Neurons, Afferent - metabolism Neuropharmacology Pharmacology. Drug treatments Rats Receptors, Drug - antagonists & inhibitors Receptors, Drug - metabolism Thiourea - chemistry Thiourea - metabolism Thiourea - pharmacology
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Zusammenfassung:	A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. ( R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC 50 value of 0.05 μM which is 10-fold more potent than capsazepine. Chain-branching led to a significant change in the mode of action and the potency against vanilloid receptor 1.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.01.066