57382-10-2Relevant academic research and scientific papers
Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists
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
, p. 1751 - 1755 (2007/10/03)
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 IC50 value of 0.05 μM which is 10-fold more potent than capsazepine.
COX-1/COX-2 inhibitors based on the methanone moiety
Dannhardt, Gerd,Fiebich, Bernd L,Schweppenhaeuser, Johannes
, p. 147 - 161 (2007/10/03)
This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors. Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl methanone element was chosen as a lead. Modifications were carried out on this scaffold to obtain potent inhibitors of the COX enzymes. The N-(2-aroylphenyl)sulphonamides and -amides were studied in detail, and to consolidate the data evaluated the corresponding 3- and 4-regioisomers were also investigated. The potency and the enzyme selectivity were varied by structural modifications of the lead.
