289903-33-9Relevant articles and documents
Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics
Lee, Jeewoo,Lee, Jiyoun,Kang, Myung-Sim,Kim, Kang-Pil,Chung, Suk-Jae,Blumberg, Peter M.,Yi, Jung-Bum,Park, Young Ho
, p. 1171 - 1179 (2007/10/03)
In order to improve the analgesic activity and pharmacokinetics of thioureas 2 and 3, which we previously developed as potent vanilloid receptor (VR) agonists, we prepared and characterized phenolic modifications of them and of their amide surro-gates (7, 8). The aminoethyl analogue of the amide template 13 was a potent analgesic with an EC50 =0.96 μg/kg in the AA-induced writhing test and with better in vivo stability than the parent phenol. Copyright