A series of substituted imidazoline derivatives were synthesized and characterized. Compounds were tested in-vivo for their antihypertensive, analgesic, antiaggressive, depressant, antidepressant, and ALD activities. The compounds 3a, 3c, 4c, 5a, and 6c showed cardiovascular as well as central nervous system activities and are potential candidate as drug among all fifteen compounds tested. All these compounds have shown better activity for antihypertensive, analgesic, antiaggressive, and depressant-antidepressant, properties than reference compounds clonidine, morphine, diazepam, and imipramine respectively. Most of the compounds have shown ALD > 500 mg/kg with maximum in 4a and 5a (>1000 mg/kg).
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http://dx.doi.org/10.1016/j.bmcl.2020.127595 | DOI Listing |
Anticancer Agents Med Chem
February 2025
School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products; Kunming Medical University, 1168 Western Chunrong Road, Yuhua Street, Chenggong District, Kunming City, Yunnan 650500, P. R. China.
The p53 protein, renowned as the "anti-cancer protein," plays a critical role in regulating the cell cycle, inducing apoptosis, and repairing DNA. Its dysregulation often leads to genomic instability and tumorigenesis. MDM2, a key negative feedback regulator of p53, inhibits both the transcriptional activity and stability of p53, thereby suppressing the anti-cancer effect of p53.
View Article and Find Full Text PDFBMJ Case Rep
February 2025
Internal Medicine, Western Michigan University Homer Stryker MD School of Medicine, Kalamazoo, Michigan, USA.
Tizanidine, a muscle relaxant, exerts its mechanism as a centrally acting alpha-2 adrenergic receptor agonist and binds to imidazoline receptors. Bradycardia and hypotension are adverse effects associated with alpha-2 adrenergic receptor agonists. A man in his 50s with a medical history of hypertension and chronic back pain presented with chest pain and hypertension.
View Article and Find Full Text PDFNat Commun
February 2025
Key Laboratory of Green Chemistry & Technology Ministry of Education, College of Chemistry Sichuan University, Chengdu, 610064, China.
Compared with rare-earth (RE)…heteroatom interaction, RE…π interaction, frequently used in facilitating regio- and stereoselectivity of olefin polymerizations, is seldomly used to trigger catalytic C - H functionalization. Here, we describe a direct anti-Markovnikov hydroallylation reaction of styrene derivatives with 1-aryl-2-alkyl alkenes and α-alkenes by use of RE…π interaction. This protocol provides a straightforward and atom-efficient route for the synthesis of valuable chain elongated internal alkenes (65 examples, up to 99% yield, > 19:1 E/Z ratio).
View Article and Find Full Text PDFChemistry
February 2025
Catalyse Organométallique, Synthèse Organique et Santé, Institut de Chimie, UMR 7177 CNRS, Université de Strasbourg, 4 rue Blaise Pascal, 67070, Strasbourg, France.
A series of chiral *Flu-NHC-gold(I) complexes, where *Flu-NHC is an N-heterocyclic carbene (imidazolin-2-ylidene or benzimidazolin-2-ylidene) bearing a chiral 9-alkyl-9-fluorenyl N-substituent and a 2,6-diisopropylphenyl or benzyl N'-substituent, were straightforwardly prepared in few steps from readily available 2,6-diisopropylamine, imidazole or benzimidazole. The chirality of the N-substituent lies in the presence of a chiral alcoholic alkyl chain on the fluorenyl, which results from the opening of commercially available chiral styrene oxide, yielding to a 2-hydroxy-2-phenylethyl or a 2-hydroxy-1-phenylethyl group. Four [AuCl(*Flu-NHC)] complexes were tested as precatalysts in an enantioselective cycloisomerization of a 1,6-enyne.
View Article and Find Full Text PDFChemMedChem
February 2025
Saint Petersburg State University, 7-9-11 Universitetskaya Nab., St., Petersburg, 199034, Russian Federation.
A novel and concise approach to rare 2,3,5-triamino-imidazole scaffolds via Ni-catalyzed coupling of alkylisocyanides and N,N'-diarylguanidines has been developed. This reaction features include mild conditions (thermal or visible light activation), a wide substrate scope, and high efficiency. The coupling proceeds through a Ni/Ni catalytic cycle, involving two-electron aerobic oxidation and the sequential insertion of two isocyanide units into Ni-N bonds.
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