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Comparison of the Inhibitory Effects of Flunixin Meglumine and Meloxicam on the Smooth Muscles Motility of the Gastrointestinal Tract of Cattle.
Vet Med Sci
January 2025
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Ondokuz Mayis University, Samsun, Türkiye.
This study aimed to compare the inhibitory effect of flunixin meglumine and meloxicam on the smooth muscles of the gastrointestinal tract in male cattle. Tissue samples, including the abomasum, ileum, proximal loop and centripetal gyri of the ascending colon, were collected from routinely slaughtered male cattle. These samples were sectioned into strips and mounted in an isolated tissue bath system.
View Article and Find Full Text PDFFinerenone: a breakthrough mineralocorticoid receptor antagonist for heart failure, diabetes and chronic kidney disease.
Egypt Heart J
December 2024
Department of Cardiology, Sanjay Gandhi Post Graduate Institute of Medical Sciences, Lucknow, Uttar Pradesh, 226014, India.
Background: Aldosterone is categorized as a mineralocorticoid hormone produced in the zona glomerulosa of the adrenal cortex. Aldosterone has considerable action in sodium and water retention along with cardiac remodeling, promoting fibrosis and these detrimental effects have been counteracted by mineralocorticoid receptors antagonists over time. Spironolactone, a non-selective steroidal MRA used extensively is potent but has serious adverse effects like gynecomastia and hyperkalemia.
View Article and Find Full Text PDFNovel isatin conjugates endowed with analgesic and anti-inflammatory properties: design, synthesis and biological evaluation.
Future Med Chem
January 2025
Department of Chemistry and Biochemistry, Augusta University, Augusta, GA, USA.
Aims: This study aimed to develop novel molecular hybrid conjugates integrating isatin, rhodanine, and phthalimide pharmacophores to create effective analgesic and anti-inflammatory agents with improved safety profiles over existing treatments.
Materials & Methods: A series of hybrid conjugates () were synthesized and evaluated through in vitro and in vivo biological assays. The most promising compound, , underwent extensive pharmacological and toxicological evaluations.
2-Trifluoromethyl-2H-chromene ethers: The dual triumph of anti-inflammation and analgesia with minimal ulcer threat.
Bioorg Chem
January 2025
State Key Laboratory of Fine Chemicals, Department of Pharmaceutical Engineering, School of Chemical Engineering, Dalian University of Technology, 2 Linggong Road, Dalian 116024, PR China. Electronic address:
In this report, we disclose the design and synthesis of a series of 2-trifluoromethyl-2H- chromene ethers as novel COX-2 inhibitors with low ulcerogenicity. Among them, 6-fluoro-3-(4-methoxyphenyl)-2-(2-(thiophen-3-yl)ethoxy)-2-(trifluoromethyl)-2H-chromene (E25) significantly suppressed LPS-induced release of NO and PGE, expression of COX-2 and iNOS, and activation of NF-κB pathway. The inhibitory effect of E25 on human recombinant COX-2 (IC = 70.
View Article and Find Full Text PDFEnzyme-Catalyzed Dynamic Kinetic Resolution for the Asymmetric Synthesis of 2,3-Dihydrobenzofuran Esters and Evaluation of Their Anti-inflammatory Activity.
Org Lett
December 2024
School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
Utilizing enzymes as biocatalysts, an alternative strategy has been developed for the highly enantioselective synthesis of chiral 2,3-dihydrobenzofuran (2,3-DHB) esters via the dynamic kinetic resolution of 2,3-dihydro-3-benzofuranols, which are generated from an intramolecular Aldol reaction. This protocol provides easy access to a series of 2,3-DHB ester derivatives, prodrugs, and allows for functional group transformations. Biological evaluation also indicates that some of the products exhibit potent anti-inflammatory activity.
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