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Discovery of a Novel p38α-MK2 Complex Inhibitor as a Potential Choice for Autoimmune Diseases.
J Med Chem
January 2025
Chemical Pharmaceutical Research Center, Changchun GeneScience Pharmaceutical Co., Ltd., Shanghai 200120, P.R. China.
The p38α-MK2 signaling axis plays an important role in the inflammatory response of cells. Here, we carried out a series of optimizations on CDD-450, aiming to enhance inhibition of the p38α-MK2 complex and improve pharmacokinetic properties. First, the magic F strategy was utilized to obtain compound , which displayed a 60-fold increase in tumor necrosis factor α inhibition and a 600-fold increase in interleukin-6 inhibition.
View Article and Find Full Text PDFIn Vitro Study of Antiviral Properties of Compounds Based on 1,4-Dioxane Derivative of Closo-Decaborate Anion with Amino Acid Ester Residues Against Influenza Virus A/IIV-Orenburg/83/2012(H1N1)pdm09.
Molecules
December 2024
Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Moscow 119991, Russia.
New derivatives of the -decaborate anion [BH-O(CH)O(CH)C(O)-L-OCH] (An) (: L = Trp; : L = His; : L = Met; : L = Ala(2-oxopyrrolidin-3-yl) (Pld) were synthesized and isolated as tetraphenylphosphonium salts (PhP)An. Anions ; ; , and contain a pendant functional group from the L-tryptophan methyl ester, L-histidine methyl ester, L-methionine methyl ester, or methyl 2-amino-3-(2-oxopyrrolidin-3-yl)propanoate (-Trp-OCH, -His-OCH, -Met-OCH, or -Pld-OCH) residue, respectively, bonded with the boron cluster anion through the oxybis[(ethane-2,1-diyl)oxy] spacer. This pacer is formed as a result of the nucleophilic opening of the attached dioxane molecule in the [BHO(CH)O] starting derivative.
View Article and Find Full Text PDFDeep learning-based discovery of compounds for blood pressure lowering effects.
Sci Rep
January 2025
School of Pharmacy, Guilin Medical University, Guilin, 541199, China.
The hypotensive side effects caused by drugs during their use have been a vexing issue. Recent studies have found that deep learning can effectively predict the biological activity of compounds by mining patterns and rules in the data, providing a potential solution for identifying drug side effects. In this study, we established a deep learning-based predictive model, utilizing a data set comprised of compounds known to either elevate or lower blood pressure.
View Article and Find Full Text PDFAmorphous Solid Dispersions of Glycyrrhetinic Acid: Using Soluplus, PVP, and PVPVA as the Polymer Matrix to Enhance Solubility, Bioavailability, and Stability.
AAPS PharmSciTech
December 2024
Hebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, 067000, Hebei, China.
Glycyrrhetinic acid (GA) possesses various pharmacological effects, including anti-inflammatory, anti-tumor, and anti-viral properties. However, its clinical application is limited by poor solubility and low oral bioavailability. Polymers play a crucial role in pharmaceutical formulations, particularly as matrices in excipients to enhance the solubility, bioavailability, and stability of active pharmaceutical ingredients.
View Article and Find Full Text PDFAntiviral Activity of (1,9a)-1-[(1,2,3-Triazol-1-yl)methyl]octahydro-1-quinolizines from the Alkaloid Lupinine.
Molecules
December 2024
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Influenza is a disease of significant morbidity and mortality. The number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. This article presents the results of assessing the antiviral activity of 1,2,3-triazole-containing derivatives of alkaloid lupinine for their ability to suppress the reproduction of orthomyxoviruses (influenza viruses: A/Vladivostok/2/09 (H1N1) and A/Almaty/8/98 (H3N2)).
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