In this communication we describe a novel strategy for the formation of valuable diaryl and aryl alkyl ketones from acyl hydrazides. A wide variety of ketones are prepared and the mild reaction conditions allow for the use of a range of functionalities, especially in the synthesis of diaryl ketones.
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http://dx.doi.org/10.1039/c3cc47967f | DOI Listing |
ACS Appl Mater Interfaces
January 2025
Oil & Gas Field Applied Chemistry Key Laboratory of Sichuan Province, College of Chemistry and Chemical Engineering, Southwest Petroleum University, Chengdu 610500, China.
In this study, waste polystyrene was modified and upgraded to prepare formylated polystyrene, and the modified polystyrene acetyl hydrazone (LT-HPA) was synthesized by condensation with polymethyl-propionyl-hydrazine. It is proven that the modification of the adsorption material is successful by various characterization methods. In the subsequent pollutant removal study, pH, mass, concentration, contact time, and salt ion interference were investigated.
View Article and Find Full Text PDFEur J Pharm Sci
February 2025
Departamento de Química e Bioquímica, Faculdade de Ciências, Centro de Química Estrutural, Institute of Molecular Sciences, Universidade de Lisboa, Campo Grande 1749-016, Portugal. Electronic address:
Tuberculosis is one of the leading causes of mortality worldwide due to the growth of multi-drug resistant strains unsusceptible to currently available therapies. Four compounds, isoniazid (INH) and three derivatives, N'-decanoylisonicotinohydrazide (INHC10), N'-(E)-(4-phenoxybenzylidene)isonicotinohydrazide (N34) and N'-(4-phenoxybenzyl)isonicotinohydrazide (N34red), were studied. Owing to their advantageous in vitro selectivity index against the primary mutation responsible for drug resistance in Mycobacterium tuberculosis (Mtb), as well as their suitable lipophilicity and interaction with human serum albumin, INHC10 and N34 were deemed promising antitubercular compounds.
View Article and Find Full Text PDFJ Org Chem
December 2024
Pfizer Oncology Medicinal Chemistry, San Diego, California 92121, United States.
A 3-step modular procedure combining carboxylic acids with acyl hydrazines provides access to medicinally relevant [1,2,4]-fused triazoles. Good to excellent yields are achieved with tolerance of aliphatic and aryl substituents as well as 5-, 6-, and 7-membered rings for the fused ring. Conditions that can avoid column chromatography and be applicable for both small scale discovery efforts as well as large scale development processes are demonstrated within.
View Article and Find Full Text PDFBioorg Med Chem
December 2024
Department of Environmental Health Sciences, University of Michigan, Ann Arbor, MI 48109, USA; Department of Neurology, University of Michigan, Ann Arbor, MI 48109, USA; Center of Computational Medicine and Bioinformatics, University of Michigan, Ann Arbor, MI 48109, USA; Michigan Institute for Computational Discovery and Engineering, University of Michigan, Ann Arbor, MI 48109, USA; Michigan Institute for Data and AI in Society, University of Michigan, Ann Arbor, MI 48109, USA. Electronic address:
A series of 2-arylhydrazinylidene-3-oxo acids (AHOAs) was prepared by dealkylation of alkyl-2-arylhydrazinylidene-3-oxo-3-alkanoates with AlBr. Using X-Ray, NMR spectroscopy, and quantum mechanical calculations (QM), the existence of AHOAs in a thermodynamically favorable Z-form stabilized by two intramolecular H-bonds was established. All AHOAs had acceptable ADME parameters.
View Article and Find Full Text PDFCureus
September 2024
Department of Pharmaceutical Chemistry, Saveetha College of Pharmacy, Saveetha Institute of Medical and Technical Sciences, Chennai, IND.
Objective The study's goal was to come up with and make a new group of 1,3,4-oxadiazole derivatives (3a-3e) and test how well they could kill (Mtb) H37Rv strain. Additionally, molecular docking and pharmacokinetic properties were analyzed using computational software to identify potential inhibitors, followed by in vitro antimycobacterial assays. Methods A group of 1,3,4-oxadiazoles was prepared by reacting acyl hydrazides with alanine, an N-protected α-amino acid, and a small amount of POCl.
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