Novel 1,2-diaryl-1-ethanone 1 and pyrazolo [4,3-c] quinoline-4-one 2, with pharmacophores different from the known COX inhibitors were identified as selective COX-2 inhibitors. The communication briefly describes SAR of both the series.
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http://dx.doi.org/10.1016/j.bmcl.2003.10.052 | DOI Listing |
Org Biomol Chem
January 2025
Institute of Natural Sciences and Mathematics, Ural Federal University, 51 Lenina Ave., 620000 Ekaterinburg, Russian Federation.
The labile tautomerism of -unsubstituted 5-acyl-4-pyridones, which exist in the form of 4-pyridone or 4-hydroxypyridine depending on the solvent, has been demonstrated. This equilibrium determines the reactivity of pyridones and their ability to undergo substitution reactions of the OH group. A regioselective and convenient method for the construction of functionalized pyrazolo[4,3-]pyridines (30-93%) based on the intramolecular amination reaction of 4-pyridones with hydrazines has been developed.
View Article and Find Full Text PDFIntroduction: Systemic lupus erythematosus (SLE) is a chronic inflammatory autoimmune disease that affects various body systems, including the skin and facial features. Estrogen promotes lupus in human and mouse models of SLE. In this study, we conducted an in vivo study to investigate the relationship between two estrogen receptors (ERα and ERβ) and platelet-activating factor acetylhydrolase (PAF-AH) on the symptoms of SLE.
View Article and Find Full Text PDFis the most common cause of life-threatening fungal infection in the developed world but remains a therapeutic challenge. Protein kinases have been rewarding drug targets across diverse indications but remain untapped for antifungal development. Previously, screening kinase inhibitors against revealed a 2,3-aryl-pyrazolopyridine, GW461484A (GW), which targets casein kinase 1 (CK1) family member Yck2.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Department of Chemistry, Key Laboratory of Surface & Interface Science of Polymer Materials of Zhejiang Province, Zhejiang Sci-Tech University, Hangzhou, Zhejiang 310018, P. R. China.
An atmospheric oxygen-mediated oxidative coupling of primary and secondary alcohols for the synthesis of nitrogen-containing heterocycles has been developed. This method utilizes atmospheric oxygen as the sole, environmentally friendly oxidant to convert a variety of alkyl and aromatic primary alcohols into aldehyde equivalents, avoiding over-oxidation to carboxylic acids. Notably, these mild oxidation conditions are compatible with both primary and secondary alkyl alcohols as substrates.
View Article and Find Full Text PDFBioorg Chem
January 2025
Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221005, India; Glycochemistry Laboratory, School of Physical Sciences, Jawaharlal Nehru University, New Delhi 110067, India. Electronic address:
Molecular hybridization is an emerging strategy in medicinal chemistry for designing new bioactive molecules that link pharmacophores covalently and shows synergistic enhanced properties. Herein, we have developed pyrazolo[3,4-b]pyridine-based new glycohybrids considering the Warburg effect. A microwave-assisted, copper-catalyzed efficient synthesis of new triazole-linked glycohybrids based on pyrazolo[3,4-b]pyridines scaffold was achieved successfully in high yields with inherent stereochemical diversity from d-glucose, d-galactose, and d-mannose.
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