We are reporting herein for the first time the synthesis of α-aminophosphonates containing Indazole moiety in two steps. In the first step, imines of substituted N-benzylidene-1-methyl-1H-indazole-3-carbohydrazide are synthesized and in the next step it has converted to α-aminophosphonates using chlorotrimethylsilane (TMSCl) and triethyl phosphite. Some of the synthesized derivatives are evaluated for antibacterial activity against different bacterial strains.
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http://dx.doi.org/10.1016/j.ejmech.2012.01.024 | DOI Listing |
Chem Asian J
January 2025
Northwest University, Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, Department of Chemistry & Materials Science,, 1 Xuefu Ave., Guodu Education and Hi-Tech Industries Zone,, Chang'an District, 710127, Xi'an, CHINA.
Herein, we describe a protocol for Brønsted acid-catalyzed regioselective coupling of azoles such as pyrazoles, 1,2,3-triazole, 1,3,4-triazole, benzotriazole, indazole and tetrazole, to cyclobutenes. These azoles could be directly coupled with various arylcyclobutenes with high site-selectivity, offering a distinct entry to more functionalized cyclobutanes. The usage of inexpensive TsOH•H2O catalyst, broad substrate scope, and open-air conditions make this protocol practically viable.
View Article and Find Full Text PDFBioorg Chem
January 2025
Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, 605 Fenglin Road, Nanchang, Jiangxi, 330013, China. Electronic address:
Anaplastic lymphoma kinase (ALK) and tyrosine protein kinase (ROS1) are recognized as driver genes in lung cancer, with dual inhibition of both targets offering a promising approach to enhance therapeutic outcomes in non-small cell lung cancer (NSCLC). Although numerous ALK/ROS1 inhibitors have received FDA approval, detailed research into the essential active structural motifs within these inhibitors remains limited. Addressing this gap, the current study employed computer-aided drug design (CADD) methodologies, incorporating bioisosteric and conformational similarity principles to design and synthesize 31 dual-target 2-morpholinobenzamide derivatives.
View Article and Find Full Text PDFGenes Environ
November 2024
Global Drug Safety, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba-shi, Ibaraki, 300-2635, Japan.
Background: Although the in silico predictive ability of the Ames test results has recently made remarkable progress, there are still some chemical classes for which the predictive ability is not yet sufficient due to a lack of Ames test data. These classes include simple heterocyclic compounds. This study aimed to investigate the mutagenicity and structure-mutagenicity relationships for some heterocycles in the Ames test.
View Article and Find Full Text PDFChemistryOpen
December 2024
Department of Physics, Chemistry and Biology, Linköping University, SE-581 83, Linköping, Sweden.
bioRxiv
October 2024
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, Bouvé College of Health Sciences, Center for Drug Discovery, Northeastern University, Boston, Massachusetts 02115, United States.
Synthetic cannabinoid receptor agonists (SCRAs) represent a class of new psychoactive substances that pose great health risks attributed to their wide-ranging and severe adverse effects. Recent evidence has shown that SCRAs with key moieties can confer superagonism, yet this phenomenon is still not well understood. In this study, we developed a structure-activity relationship (SAR) for SCRA superagonism by comparing eight compounds differing by their head moiety (l-valinate vs.
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