Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: Structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents
- Authors
- Suh, YG; Lee, YS; Min, KH; Park, OH; Kim, JK; Seung, HS; Seo, SY; Lee, BY; Nam, YH; Lee, KO; Kim, HD; Park, HG; Lee, J; Oh, U; Lim, JO; Kang, SU; Kil, MJ; Koo, JY; Shin, SS; Joo, YH; Kim, JK; Jeong, YS; Kim, SY; Park, YH
- Issue Date
- Sep-2005
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.48, no.18, pp 5823 - 5836
- Pages
- 14
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 48
- Number
- 18
- Start Page
- 5823
- End Page
- 5836
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/15475
- DOI
- 10.1021/jm0502790
- ISSN
- 0022-2623
1520-4804
- Abstract
- Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure- activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM.
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