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Silicon switch approach in TRPV1 antagonist MK-056 and its analogues
- Chang, Minsun;
- Park, Seol-Rin;
- Kim, Juhyun;
- Jang, Mijung;
- Park, Jeong Hyun;
- 외 6명
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8초록
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.
키워드
Silicon switch; TRPV1; Antagonist; 1,3-Dibenzylthiourea; VANILLOID RECEPTOR TRPV1; CAPSAICIN RECEPTOR; CHANNEL; CHEMISTRY; POTENT; THIOUREAS; TARGET
- 제목
- Silicon switch approach in TRPV1 antagonist MK-056 and its analogues
- 저자
- 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
- 발행일
- 2010-01-01
- 유형
- Article
- 권
- 18
- 호
- 1
- 페이지
- 111 ~ 116