44 research outputs found
Ligand-free Cu-catalyzed O-arylation of aliphatic diols
No full textCoupling reaction between aryl iodides and aliphatic diols was realized with a ligand-free copper catalyst under mild conditions. This method was successfully applied in the process of scale-up synthesis of medicinal candidate product EMB-3.Ministry of Science and Technology of China [2012ZX09103101-042]SCI(E)[email protected]
Synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums
No full textA series of proline derivated spirocyclic quaternary ammoniums were synthesized and evaluated via in vivo analgesic activities. Compounds 9a showed the best analgesic effect with 84 % inhibition in mice. These compounds showed only micromolar Ki value by in vitro alpha 7 nAChR binding test, which may indicate the form of active metabolite play a role in their in vitro analgesic activities.http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000330766600028&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=8e1609b174ce4e31116a60747a720701Chemistry, MedicinalSCI(E)[email protected]; [email protected]
A low-power-consumption and high efficiency security system for automatic detection of concealed objects in human body
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Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors
No full textA series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available substances in moderate to good yields. All of these N-heterocyclic compounds were characterized by nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) analysis and tested for phosphoinositide 3-kinase (PI3K) enzymatic assay. The results indicated that these N-heterocyclic compounds showed potent PI3K inhibitory activity, and the IC50 of a representative compound (19a) could reach to 3.6 nm. The structure−activity relationships (SAR) study showed that sulfonamide functionality was important for PI3Kα inhibitory activity, and 2-chloro-4-florophenyl sulfonamide (19b), or 5-chlorothiophene-2-sulfonamide (19c) showed potent inhibitory activity with a nanomolar IC50 value. The pyridyl attached to thiazolo[5,4-b]pyridine was another key structural unit for PI3Kα inhibitory potency, and replacement by phenyl lead to a significant decrease in activity. Enzymatic Inhibition results showed that compound 19a inhibited PI3Kα, PI3Kγ, or PI3Kδ with a nanomolar IC50 value, but its inhibitory activity on PI3Kβ was approximately 10-fold reduced. Further docking analysis revealed that the N-heterocyclic core of compound 19a was directly involved in the binding to the kinase through the key hydrogen bonds interaction
A Literature Review on Maillard Reaction Based on Milk Proteins and Carbohydrates in Food and Pharmaceutical Products: Advantages, Disadvantages, and Avoidance Strategies
No full textMilk has two main components that have high nutritional value—milk protein (casein and whey protein), and lactose. These components are extensively used in various areas, especially in food, i.e., as sweeteners, stabilizers, functional food ingredients, nutritional fortifiers, etc. Non-enzymatic browning refers to a series of chemical reactions between sugars and proteins that make food more appetizing. Non-enzymatic browning reactions include degradation of ascorbic acid, lipid peroxidation, caramel reaction, and the Maillard reaction (MR). The MR, as one of the four non-enzymatic browning reactions, has been well studied and utilized in food fields. Milk protein and lactose, as two main components of milk, have high chemical activities; they are used as reactants to participate in the MR, generating Maillard reaction products (MRPs). The MR involves a condensation reaction between carbonyl groups of various sugars and amino groups of amino acids/proteins. These MRPs have different applications in various areas, including food flavor, food oxidation resistance, drug carriers, etc. This work presents the positive and negative effects of the MR, based on the two main components of milk, used in food and medicine, as well as avoidance approaches to prevent the occurrence of negative effects
