Ryu Chong Hyun, Jang Mi Jung, Jung Jeong Wha, Park Ju-Hyun, Choi Hye Young, Suh Young-Ger, Oh Uhtaek, Park Hyeung-Geun, Lee Jeewoo, Koh Hyun-Joo, Mo Joo-Hyun, Joo Yung Hyup, Park Young-Ho, Kim Hee-Doo
College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Republic of Korea.
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1751-5. doi: 10.1016/j.bmcl.2004.01.066.
A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. (R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC(50) value of 0.05 microM which is 10-fold more potent than capsazepine.
合成了一系列链支化的1,3 - 二苄基硫脲衍生物，并测试了它们对香草酸受体1的拮抗活性。链支化导致作用方式和效力发生显著变化。(R)-甲基或乙基支化的1,3 - 二苄基硫脲衍生物表现出最强的拮抗活性，其IC(50)值高达0.05微摩尔，比辣椒素受体拮抗剂强10倍。
