1128-28-5Relevant articles and documents
Synthesis, characterizations, biological activities and docking studies of novel dihydroxy derivatives of natural phenolic monoterpenoids containing azomethine linkage
Rajput, Jamatsing D.,Bagul, Suresh D.,Hosamani, Amar A.,Patil, Manohar M.,Bendre, Ratnamala S.
, p. 5377 - 5393 (2017)
Abstract: In the present work, we report the synthesis of six new azomethine linkage containing dihydroxy derivatives of carvacrol, thymol, and eugenol. All the synthesized derivatives have been characterized by spectroscopic techniques and their structures were confirmed by X-ray single crystallography. Synthesized derivatives were screened for anti-oxidant activity using DPPH radical scavenging assay, and anticancer activity by using SRB assay against pancreatic cancer with MIAPaCa-2 and colon cancer with HCT-15 cell lines. The molecular docking studies of all the synthesized derivatives were performed on cyclooxygenases (COX-2) protein enzyme. In the anti-oxidant test, the values of EC50 indicated that all the compounds show excellent anti-oxidant potency, and similarly the GI50 values in anticancer tests indicated that most of the compounds possess good anticancer efficacy. The overall docking score suggested that all the synthesized compounds exhibit good binding affinity towards cyclooxygenases (COX-2) protein enzyme.
[...] amine derivatives, preparation method and application thereof (by machine translation)
-
Paragraph 0052-0055, (2018/11/27)
The invention discloses a [...] amine derivatives, preparation method and its application, which belongs to the technical field of pharmaceutical chemistry. The invention thymol as parent modify, through the nitration reaction obtaining the intermediate 2 - isopropyl - 5 - methyl - 4 - nitro-phenol. On this basis to perform the derivative, prepared four [...] amine derivatives. Specific performance for introducing electronegative weaker nitrogen atom, solves the problem of further derivatization; alkylation reaction to raise the compound film breathability and bioavailability; triphenylphosphine the introduction of group enhances the drug is targeted. The final four-benzoquinone imine derivatives can eliminate the excessive reactive oxygen species in cells (ROS), and maintaining the cell in the redox balance, inhibit the oxidative stress caused by the inflammation reaction; and can effectively induce apoptosis of inflammatory cells, to reduce inflammation reaction effect cell, demonstrate a certain anti-inflammatory superior pharmacological activity. (by machine translation)
The Diels-Alder reactions of para-benzoquinone nitrogen-derivatives: An experimental and theoretical study
Uliana, Marciana P.,Servilha, Bruno M.,Alexopoulos, Olga,De Oliveira, Kleber T.,Tormena, Cláudio F.,Ferreira, Marco A.B.,Brocksom, Timothy J.
, p. 6963 - 6973 (2015/11/09)
An experimental and theoretical study of the comparative reactivity and selectivity of the Diels-Alder reactions of para-benzoquinones and three nitrogen derivatives have been performed. The mono-oximes derivatives do not react under the tested reaction conditions, whereas the tosylated mono-oximes react slowly. However, the mono N-tosyl imines show excellent reactivity, and superior to the parent parabenzoquinones. DFT calculations support these experimental results.