Author/Authors :
Minsun Chang، نويسنده , , Seol-Rin Park، نويسنده , , Juhyun Kim، نويسنده , , Mijung Jang، نويسنده , , Jeong-Hyun Park، نويسنده , , Ji-Eun Park، نويسنده , , Hyeung-geun Park، نويسنده , , Young-Ger Suh، نويسنده , , Yeon Su Jeong، نويسنده , , Young-Ho Park، نويسنده , , Hee-Doo Kim، نويسنده ,
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 μM, 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.
Keywords :
Silicon switch , Antagonist , 1 , 3-Dibenzylthiourea , TRPV1
