122019-53-8Relevant articles and documents
AROMATIC ACETYLENE OR AROMATIC ETHYLENE COMPOUND, INTERMEDIATE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Paragraph 0140; 0208; 0210, (2019/05/22)
Disclosed are an aromatic acetylene or aromatic ethylene compound, an intermediate, a preparation method, a pharmaceutical composition and a use thereof. The aromatic acetylene or aromatic ethylene compound has a significant inhibitory effect on PD-1 and PD-L1, and can effectively relieve or treat cancers and other related diseases.
Evaluation and Synthesis of Aminohydroxyisoxazoles and Pyrazoles as Potential Glycine Agonists
Drummond, J.,Johnson, G.,Nickell, D. G.,Ortwine, D. F.,Bruns, R. F.,Welbaum, B.
, p. 2116 - 2128 (2007/10/02)
Except for structurally similar small amino acids, such as alanine, β-alanine, and serine, compounds acting as glycine-receptor agonists are an unknown class of pharmacological agents.To investigate the potential of small, substituted heterocycles to act as glycine agonists, we have evaluated the similarities between glycine and a series of hydroxy- and amino-substituted pyrazoles and isoxazoles through complementary molecular modeling techniques.Using a "scorecard approach" to determine the overall similarity of projected agonist structures to glycine, we prioritized synthesis and subsequently prepared several novel derivatives.The biological activity of these compounds was compared to that of glycine by using a strychnine-mediated glycine receptor binding assay.Despite the close similarity in the calculated parameters when compared to glycine, no significant receptor-binding activity was observed for the targeted analogues.These results illustrate the structurally exacting nature of the glycine receptor.