161992-97-8Relevant academic research and scientific papers
Modeling of controlled release of aspirin derivatives from human erythrocytes
Ohsako,Oka,Tsuzuki,Matsumoto
, p. 310 - 314 (1995)
The transport of aspirin (ASP) and its derivatives (m- or p-acetoxybenzoic acid (m- or p-AcOHBA), o-propionyloxybenzoic acid (PrOHBA), o-butyryloxybenzoic acid (BuOHBA), o-acetoxyhippuric acid (AcOHPA), and o-acetoxy-N-benzoyl-β-alanine (AcONBA)) through
Synthesis and biological evaluation of the codrug of Leonurine and Aspirin as cardioprotective agents
Gao, Huan,Yang, Xiaohong,Gu, Xianfeng,Zhu, Yi-Zhun
, p. 4650 - 4654 (2016)
The novel codrugs of Leonurine and Aspirin, compounds 545 and 503 have been synthesized and evaluated on their cardioprotective effects. Preliminary pharmacological studies showed that both compounds 545 and 503 were able to increase cell viability of hypoxia-induced H9c2 cells, and compound 545 exhibited at least ten fold potency than 503 and their parent drugs (Leonurine and Aspirin). Further mechanisms studies indicated that the cardioprotective effect of 545 due to its (1) anti-oxidative ability by increasing SOD and CAT enzymes activity and decreasing MDA content and LDH leakage rate, (2) anti-apoptosis activity by regulating apoptosis-associated proteins expression during hypoxia, (3) anti-inflammatory effect by suppression of pro-inflammatory mediators. All of these results demonstrate that compound 545 as a new class of Leonurine analogue could be a drug candidate in our further drug development studies.
Preparation method of leonurine and aspirin conjugate
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Paragraph 0051-0053, (2017/04/19)
The invention belongs to the field of medicinal chemistry, and relates to a synthesizing method of leonurine and aspirin conjugate. The method comprises the steps that syringic acid, S-methylisothiourea and aspirin serve as starting materials, reactions o
Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin
Leone-Bay, Andrea,Paton, Duncan R.,Freeman, John,Lercara, Christine,O'Toole, Doris,Gschneidner, David,Wang, Eric,Harris, Elizabeth,Rosado, Connie,Rivera, Theresa,DeVincent, Aldonna,Tai, Monica,Mercogliano, Frank,Agarwal, Rajesh,Leipold, Harry,Baughman, Robert A.
, p. 1163 - 1171 (2007/10/03)
A family of novel compounds (delivery agents) that promote the gastrointestinal absorption of USP heparin in rats and primates has been discovered. The delivery agents in combination with heparin were administered either orally or intracolonically in an aqueous propylene glycol solution and caused dramatic increases in both plasma heparin concentrations (anti-Factor Xa) and clotting times (APTT). Using one of the most effective delivery agents in this series, an estimated relative bioavailability of 8% can be achieved following oral administration to cynomolgus monkeys. To establish a correlation between the in vivo data and an in vitro parameter, immobilized artificial membrane (IAM) chromatography was performed. Log relative k' values were correlated to the efficiency of oral heparin delivery.
