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Silicon switch approach in TRPV1 antagonist MK-056 and its analogues
- Authors
- Chang, Minsun; Park, Seol-Rin; Kim, Juhyun; Jang, Mijung; Park, Jeong Hyun; Park, Ji Eun; Park, Hyeung-Geun; Suh, Young-Ger; Jeong, Yeon Su; Park, Young-Ho; Kim, Hee-Doo
- Issue Date
- 1-Jan-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Silicon switch; TRPV1; Antagonist; 1,3-Dibenzylthiourea
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.1, pp 111 - 116
- Pages
- 6
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 18
- Number
- 1
- Start Page
- 111
- End Page
- 116
- ISSN
- 0968-0896
1464-3391
- Abstract
- In searching for opportunities to exploit the benefits of silicon in TRPV1 research, we tried to investigate the pharmacological effects of sila-substitution (C/Si exchange) of tert-butyl group in the MK-056 series. Compound 13a, with a 4-positioned trimethylsilanyl group on the B ring in place of tert-butyl group, exhibited the most potent antagonist activity with IC50 values of 0.15 mu M, which is almost equipotent with that of MK-056. This is the first example that tert-butyl group on MK-056 series can be replaced to the other substituent without loss of activity. (C) 2009 Elsevier Ltd. All rights reserved.
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