A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action.
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http://dx.doi.org/10.1016/s0960-894x(02)00249-4 | DOI Listing |
J Agric Food Chem
January 2025
Instituto de Química, Laboratório de Química Metodológica e Orgânica Sintética (LaQMOS), Universidade de Brasília, 70904-970 Brasília, DF, Brazil.
In this work, several imidazo[1,2-]pyridines were synthesized through the Groebke-Blackburn-Bienaymé three-component reaction (GBB-3CR), and their phytotoxicity was evaluated by the influence on the growth of wheat coleoptiles and three important agricultural seeds (, , and ) at test concentrations of 1000, 300, 100, 30, and 10 μM. A structure-activity relationship was established, showing the importance of halogen groups at the position of the attached aromatic ring and the presence of a cyclohexylamine group for greater activity. Post-modification of some GBB-3CR adducts was carried out, leading to imidazo[1,2-]pyridine-tetrazole hybrids, which were also evaluated in these bioassays.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
Medical Research Center, Oulu University Hospital, Oulu, Finland; Department of Internal Medicine, Länsi-Pohja Central Hospital, Kemi, Finland; Biomedicine and Internal Medicine Research Unit, University of Oulu, Oulu, Finland.
It has been demonstrated that diffuse large B-cell lymphoma (DLBCL) is especially sensitive to ferroptosis. Currently, confirming the presence of ferroptosis requires flow cytometry, which is a time consuming and labor-intensive task. Blistering of the cell membrane has been shown to be a ferroptosis-specific morphological change.
View Article and Find Full Text PDFBMC Microbiol
November 2024
Pharmaceutical Microbiology Department, Faculty of Pharmacy, Tanta University, Tanta, 31527, Egypt.
Int J Mol Sci
November 2024
Department of Medical Research, Chung Shan Medical University Hospital, Taichung 402, Taiwan.
Biomolecules
November 2024
The MOE Basic Research and Innovation Center for the Targeted Therapeutics of Solid Tumors, School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, Nanchang 330031, China.
Ferroptosis, a recently elucidated style of regulated cell death, has emerged as a significant area of investigation in cancer biology. Natural active compounds that have anti-cancer effects are promising candidates for cancer prevention. Iberverin, a natural compound derived from var.
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