Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 1, Pages 111-116Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.11.014
Keywords
Silicon switch; TRPV1; Antagonist; 1,3-Dibenzylthiourea
Funding
- KOSEF (Research Center for Women's Diseases)
- AmorePacific Corporation
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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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