68719-75-5Relevant academic research and scientific papers
A transition-metal-free Heck-type reaction between alkenes and alkyl iodides enabled by light in water
Liu, Wenbo,Li, Lu,Chen, Zhengwang,Li, Chao-Jun
supporting information, p. 6170 - 6174 (2015/06/08)
A transition-metal-free coupling protocol between various alkenes and non-activated alkyl iodides has been developed by using photoenergy in water for the first time. Under UV irradiation and basic aqueous conditions, various alkenes efficiently couple with a wide range of non-activated alkyl iodides. A tentative mechanism, which involves an atom transfer radical addition process, for the coupling is proposed.
Euodenine A: A small-molecule agonist of human TLR4
Neve, Juliette E.,Wijesekera, Hasanthi P.,Duffy, Sandra,Jenkins, Ian D.,Ripper, Justin A.,Teague, Simon J.,Campitelli, Marc,Garavelas, Agatha,Nikolakopoulos, George,Le, Phuc V.,De A. Leone, Priscila,Pham, Ngoc B.,Shelton, Philip,Fraser, Neil,Carroll, Anthony R.,Avery, Vicky M.,McCrae, Christopher,Williams, Nicola,Quinn, Ronald J.
, p. 1252 - 1275 (2014/03/21)
A small-molecule natural product, euodenine A (1), was identified as an agonist of the human TLR4 receptor. Euodenine A was isolated from the leaves of Euodia asteridula (Rutaceae) found in Papua New Guinea and has an unusual U-shaped structure. It was synthesized along with a series of analogues that exhibit potent and selective agonism of the TLR4 receptor. SAR development around the cyclobutane ring resulted in a 10-fold increase in potency. The natural product demonstrated an extracellular site of action, which requires the extracellular domain of TLR4 to stimulate a NF-κB reporter response. 1 is a human-selective agonist that is CD14-independent, and it requires both TLR4 and MD-2 for full efficacy. Testing for immunomodulation in PBMC cells shows the induction of the cytokines IL-8, IL-10, TNF-α, and IL-12p40 as well as suppression of IL-5 from activated PBMCs, indicating that compounds like 1 could modulate the Th2 immune response without causing lung damage.
Olefination of activated halides and mesylates using arsonium ylides
Seyer, Andre,Alcaraz, Lilian,Mioskowski
, p. 7871 - 7874 (2007/10/03)
Alkyltriphenylarsonium ylides react with activated primary halides and mesylates to afford olefins in good yields and with high E-selectivity.
Pharmacology on rat ileum of certain 2-substituted 3-(dimethylamino)-5,6-dimethoxyindenes related to 5,6-(methylenedioxy)indene calcium antagonists
Witiak,Kakodkar,Brunst,Baldwin,Rahwan
, p. 1313 - 1315 (2007/10/06)
Whereas the 2-propyl- and 2-butyl-5,6-(methylenedioxy)indene caclium antagonists reversed the spasmogenic action of several agonists including PGF(2α) and acetylcholine at 5 x 10-5 to 10-4 M on the rat ileum, the corresponding 5,6-dimethoxy analogues exhibited spasmogenic activity at higher concentration (10-4-10-3 M) and exhibited neither spasmogeric nor spasmolytic activity at lower (10-6-10-5 M) concentration. The results are compared to the methyl and 2-ethyl analogues. At 10-4 M only the butyl analogue was capable of moderate antagonism of acetylcholine and at 10-3 M all four analogues were capable of moderately antagonizing the actions of acetylcholine.
