5959-36-4Relevant articles and documents
Fluorescence PET (photo-induced electron transfer) sensor for water based on anthracene-amino acid
Ooyama, Yousuke,Matsugasako, Ai,Nagano, Tomoya,Oka, Kazuyuki,Kushimoto, Kohei,Komaguchi, Kenji,Imae, Ichiro,Harima, Yutaka
, p. 52 - 55 (2011)
An anthracene-amino acid system with two carboxyl groups has been designed and synthesized as a new class of fluorescence PET (photo-induced electron transfer) sensor for detection of water in organic solvents. An enhancement in fluorescence is observed with increasing water content in 1,4-dioxane, THF, acetonitrile and ethanol, which is attributable to the suppression of PET by the intramolecular proton transfer of the carboxyl proton to the amino group. The detection limit and quantitation limit are, respectively, 0.1 and 0.3 wt% for 1,4-dioxane, 0.4 and 1.2 wt% for THF, 0.1 and 0.3 wt% for acetonitrile and 0.1 and 0.3 wt% for ethanol.
Resveratrol amino acid ester derivative and preparation method thereof
-
Paragraph 0059; 0086-0087, (2019/07/04)
The invention discloses a resveratrol amino acid ester derivative and a preparation method thereof, and belongs to the technical field of fine chemical substance synthesis. The structure of the resveratrol amino acid ester derivative is represented by a formula shown in the description. The resveratrol amino acid ester derivative is synthesized from resveratrol, R amino acid, R' alcohol, dichlorosulfoxide and di(p-nitrobenzene) carbonate with 4-dimethylaminopyridine (DMAP) as a catalyst and acetonitrile as a solvent, wherein the R amino acid is one of alpha-alanine, beta-alanine and gamma-aminobutyric acid, and the R' alcohol is one of methanol, ethanol and n-propanol. The technical problem that resveratrol is difficult to preserve is solved, the pharmacological toxicity introduced by a resveratrol substituent group is lowered, and the resveratrol amino acid ester derivative has the pharmaceutical effects of resveratrol and amino acid. It is expected that the above novel compound playsa great role in beauty treatment and production of fatigue-relieving and blood pressure-lowering medicines.
Design, synthesis, and potent antiepileptic activity with latent nerve rehabilitation of novel γ-aminobutyric acid derivatives
He, Dian,Ma, Jing,Shi, Xiuxiao,Zhao, Chunyan,Hou, Meng,Guo, Qingxin,Ma, Shangxian,Li, Xiaojun,Zhao, Peicheng,Liu, Wenhu,Yang, Zhuqing,Mou, Jianping,Song, Pengfei,Zhang, Yang,Li, Jing
, p. 967 - 978 (2015/02/19)
We aimed to design and synthesize novel γ-aminobutyric acid (GABA) derivatives with the combination of aspirin (ASA) of nerve rehabilitative pharmacophores so as to develop multifunctional drugs useful in the treatment of neurological disorders. Twenty-four novel esters and amides of 1a were synthesized, biologically evaluated for antiepileptic activity with the model of 4-aminopyridine (4-AP), and tested for their capacity of penetrating the blood-brain barrier (BBB) with HPLC. The distribution of 8a, ASA freed by 8a, 7c, and ASA freed by 7c within 24 h in brain tissue was measured. The structure-activity relationship (SAR) was established and the data of Computer Aided Drug Design (CADD) showed good results. With ED50 values of, 0.3684-0.5199 mmol/kg, LD50 1.1487-1.3944 mmol/kg, and therapeutic index (TI) 2.65-3.15, compounds 8a, 3b, 4b, 6c, and 7c exhibited better antiepileptic activities in multiples of 0.3 to 2.2 against the control sodium valproate (VPA). Most importantly, 8a and 7c exhibited excellent antiepileptic activities with TI values of, 3.15 and 3.12, respectively.