Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents.

Bioorg Med Chem Lett

Department of Chemistry, Biochemistry & Forensic Science, Amity School of Applied Sciences, Amity University Haryana, Gurugram 122413, India. Electronic address:

Published: December 2020

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).

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2020.127595DOI Listing

Publication Analysis

Top Keywords

imidazoline derivatives
8
compounds tested
8
antihypertensive analgesic
8
analgesic antiaggressive
8
compounds
6
synthesis biological
4
biological evaluation
4
evaluation imidazoline
4
derivatives potential
4
potential cns
4

Similar Publications

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 PDF

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 PDF

Anti-Markovnikov hydroallylation reaction of alkenes via scandium-catalyzed allylic C‒H activation.

Nat 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 PDF

Chiral N-Alkylfluorenyl-Substituted N-Heterocyclic Carbenes in the Gold(I)-Catalyzed Enantioselective Cycloisomerization of 1,6-Enynes.

Chemistry

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 PDF

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.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!