124068-97-9Relevant articles and documents
Discovery of Biased Mu-Opioid Receptor Agonists for the Treatment of Pain
Ma, Mengjun,Li, Xiang,Tong, Kun,Cheng, Jingchao,Yu, Zixing,Ren, Fengxia,Zhong, Bohua,Shi, Weiguo
, p. 155 - 161 (2020)
G protein-biased mu-opioid receptor (MOR) agonists have been developed as promising new potent analgesic drugs with fewer adverse side effects than standard MOR agonists. PZM21 represents a unique chemotype unrelated to known opioids, which makes it a desirable lead for modification to find analgesics with new chemical entities. In the present study, we synthesized and tested novel PZM21 derivatives as potent biased MOR agonists by introducing a benzodioxolane group to replace the hydroxybenzene of PZM21. The new compounds displayed more potent analgesic activities in vivo and greater bias toward G protein signaling in vitro than did PZM21. These results suggest that the benzodioxolane group is essential for the maintenance of bias. Compounds 7 i ((S)-1-(3-(benzo[d][1,3]dioxol-4-yl)-2-(dimethylamino)propyl)-3-phenethylurea) and 7 j ((S)-1-(3-(benzo[d][1,3]dioxol-4-yl)-2-(dimethylamino)propyl)-3-benzylurea) could serve as new leads for further modifications to find novel biased MOR agonists with greater G protein signaling potency and less β-arrestin-2 recruitment.
A simple and efficient biphasic method for the preparation of 4-nitrophenyl N-methyl- and N-alkylcarbamates
Peterson, Matt A.,Shi, Houguang,Ke, Pucheng
, p. 3405 - 3407 (2006)
Treatment of 4-nitrophenyl chloroformate with alkylammonium hydrochloride salts and solid anhydrous Na2CO3 in either CH2Cl2 or CH3CN gave 4-nitrophenyl N-methylcarbamate and other N-alkylcarbamate ana
Biased agonist and medical application thereof
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Paragraph 0398-0402, (2021/01/24)
The invention relates to compounds shown in structural formulas I and II, stereoisomers or pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing the compounds, the stereoisomers or the pharmaceutically acceptable salts thereof as active ingredients, and uses of the compound, the stereoisomer thereof or the pharmaceutically acceptable salt thereof in preparation ofanalgesic drugs.
Reactive Oxygen Species-Triggered Tunable Hydrogen Sulfide Release
Chauhan, Preeti,Jos, Swetha,Chakrapani, Harinath
supporting information, p. 3766 - 3770 (2018/07/21)
A series of carbamothioates with tunable release of H2S after activation by reactive oxygen species are reported. The half-lives of H2S release could be tuned from 24 to 203 min by varying the basicity of the amine.