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Base-Promoted [4 + 1 + 1] Multicomponent Tandem Cycloaddition of -Substituted Nitroarenes, Aldehydes, and Ammonium Salts To Access 2,4-Substituted Quinazoline Frameworks.
J Org Chem
January 2025
Key Laboratory of Biomass Green Chemical Conversion of Yunnan Provincial Education Department, Yunnan Key La-boratory of Chiral Functional Substance Research and Application, School of Chemistry & Environment, Yunnan Minzu University, Kunming 650504, P. R. China.
We report a base-promoted, metal-free multicomponent tandem reaction, involving a [4 + 1 + 1] cycloaddition process between -substituted nitroarenes, aldehydes, and ammonium salts. Modifying the substituents on the nitroaromatic compounds effectively provides structurally diverse 2-substituted and 4-alkenylquinazolines with good to excellent yields (77%-90% and quinazoline 51 examples) and high tolerance for various inorganic ammonium salts (13 examples, such as NH·HO, NHCl, and NHHF). A new method for constructing 2,4-substituted quinazoline compounds with high selectivity from simple nitrogen source compounds was developed, and the reaction can be scaled up to a gram scale.
View Article and Find Full Text PDFSynthesis of Some Thiazolyl and Oxazolyl Quinazoline Derivatives as Potential Anti-Microbial Agents.
Curr Org Synth
January 2025
Department of Chemistry, Constituent Govt. College, (MJP. Rohilkhand University Bareilly) Hasanpur, (UP), 244241, India.
Introduction: Quinazoline holds significant importance in pharmaceutical chemistry, which is included in a range of drugs, clinical contenders, and bioactive compounds. N-contain-ing heterocyclic compounds of quinazoline have a wide and distinct range of biopharmaceutical activities.
Methods: A series of newly synthesized heterocyclic compounds, namely, N-(4-substituted ben-zylidene)-2-(2-aminothiazol-4-yl)-6-methylquinazolin-3(4H)-amines (3a'-3e') and N-(4-substi-tuted benzylidene)-2-(2-aminooxazol-4-yl)-6-methylquinazolin-3(4H)-amines (3a-3e), were synthesized starting from 6-methylquinazolin-3(4H)-amine and 4-substituted benzaldehyde and their antibacterial and antifungal properties were evaluated.
In vitro and in vivo Investigations of 4-Substituted 2-Phenylquinazoline derivatives as multipotent ligands for the treatment of Alzheimer's disease.
Bioorg Chem
February 2025
Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Central University of Punjab, Bathinda, India, 151401. Electronic address:
The pathology of Alzheimer's disease (AD) is complex due to its multifactorial nature and single targeting drugs proved inefficient. A series of novel 4-N-substituted-2-phenylquinazoline derivatives was designed and synthesized as potential multi-target directed ligands (MTDLs) through dual inhibition of AChE and MAO-B enzymes along with Aβ aggregation inhibition for the treatment of AD. Two compounds in the series, VAV-8 and VAV-19 were found to be the most potent inhibitors of both AChE and MAO-B enzymes and moderate inhibitor of Aβ, with good thermodynamic stability at the binding pocket of the enzymes.
View Article and Find Full Text PDFStructure-Guided Discovery of Novel -(Substituted Thiazol-2-yl)--(4-Substituted phenyl)pyrimidine-2,4-Diamines as Potent CDK2 and CDK9 Dual Inhibitors with High Oral Bioavailability.
J Med Chem
January 2025
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, P. R. China.
CDK2 and CDK9 play pivotal roles in cell cycle progression and gene transcription, respectively, making them promising targets for cancer treatment. Herein, we discovered a series of -(substituted thiazol-2-yl)--(4-substituted phenyl)pyrimidine-2,4-diamines as highly potent CDK2/9 dual inhibitors. Especially, compound significantly inhibited CDK2 (IC = 0.
View Article and Find Full Text PDFNovel Antimicrobial and Antitumor Agents Bearing Pyridine-1,2,4-triazole-3-thione-hydrazone Scaffold: Synthesis, Biological Evaluation, and Molecular Docking Investigation.
Biomolecules
November 2024
Department of Organic Chemistry, Kaunas University of Technology, Radvilėnų pl. 19, 50254 Kaunas, Lithuania.
A series of target 4-substituted-5-(2-(pyridine-2-ylamino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thiones and their chloro analogs - were synthesized in a reaction of the selected aldehydes with the corresponding 4-amino-1,2,4-triazole-3-thiones and , which were obtained from 3-(pyridin-2-ylamino)propanoic acid () or 3-((5-chloropyridin-2-yl)amino)propanoic acid (), respectively, with thioacetohydrazide. The antibacterial and antifungal activities of the synthesized hydrazones were screened against the bacteria , , and and the fungi and by agar diffusion and serial dilution methods. 4-Amino-5-(2-((5-chloropyridin-2-yl)amino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thione () and 4-(benzylideneamino)-5-(2-(pyridin-2-ylamino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thione () were identified as exceptionally active (MIC 0.
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