We designed the synthesis of a small library of 3-substituted-3,6-diazabicyclo[3.1.1]heptanes whose affinity on neuronal nicotinic receptors (nAChRs) was evaluated. Among the synthesized compounds, the 5-(3,6-diazabicyclo[3.1.1]heptane-3-yl)-N-(2-fluorophenyl)nicotinamide 43 proved to be the most interesting compound with αβKi value of 10 pM and a very high α/αβ selectivity. Furthermore, compounds 35, 39 and 43 elicited a selective partial agonist activity for αβ nAChR subtype. Finally, in this paper we also report the conclusions on the 3,6-diazabicyclo[3.1.1]heptanes as ligands for nAChRs, resulting from our consolidated structure activity relationship (SAR) studies on this template.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2019.06.079 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
In situ growth of defective ZIF-8 on TEMPO-oxidized cellulose nanofibrils for rapid response release of curcumin in food preservation.
Carbohydr Polym
March 2025
Liaoning Key Lab of Lignocellulose Chemistry and BioMaterials, Liaoning Collaborative Innovation Center for Lignocellulosic Biorefinery, College of Light Industry and Chemical Engineering, Dalian Polytechnic University, Dalian 116034, China. Electronic address:
Uncontrolled release of active agents in active packaging reduces antimicrobial efficacy, hindering the effective protection of perishable products from microbial infection. Herein, a novel defective engineering was proposed to design defective and hollow ZIF-8 structures grown on TEMPO oxidized cellulose nanofibrils (TOCNFs) and use them as fast-reacting nanocarriers for loading and controlled release curcumin (Cur) in sodium alginate (SA) active packaging systems (CZT-Cur-SA). By employing stable chelation between tannic acid (TA) and ZIF-8 zinc ions, the connections between zinc ions and imidazole ligands were severed to form a loose and hollow structure, which facilitates the rapid reaction and release of active ingredients triggered by pH changes in the microenvironment.
View Article and Find Full Text PDFReprint of: M1 macrophage-targeted curcumin nanocrystals with l-arginine-modified for acute lung injury by inhalation.
J Pharm Sci
January 2025
Department of Chinese Medicinal Pharmaceutics, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Yang Guang South Street, Fangshan District, Beijing 102488, China. Electronic address:
Acute Lung Injury/Acute Respiratory Distress Syndrome (ALI/ARDS) with clinical manifestations of respiratory distress and hypoxemia remains a significant cause of respiratory failure, boasting a persistently high incidence and mortality rate. Given the central role of M1 macrophages in the pathogenesis of acute lung injury (ALI), this study utilized the anti-inflammatory agent curcumin as a model drug. l-arginine (L-Arg) was employed as a targeting ligand, and chitosan was initially modified with l-arginine.
View Article and Find Full Text PDFNanocodelivery of 5-Fluorouracil and Curcumin by RGD-Decorated Nanoliposomes Achieves Synergistic Chemotherapy for Breast Cancer.
IET Nanobiotechnol
December 2024
Medicinal Plants Research Center, Yasuj University of Medical Sciences, Yasuj, Iran.
In the present study, arginine-glycine-aspartic acid peptide (RGD) surface functionalized liposomes (Lips) were formulated for the concomitant targeted delivery of two antineoplastic drugs, namely curcumin (Cur) and 5-fluorouracil (5FU) to breast cancer cells. The Lips' measured size values where 50-100 nm by transmission electron microscopy (TEM) and 169 ± 10.2 nm by dynamic light scattering (DLS), which fall within the desired range required for drug delivery purposes.
View Article and Find Full Text PDFCurcumin targets CXCL16-mediated podocyte injury and lipid accumulation in diabetic kidney disease treatment.
Arch Pharm Res
December 2024
Department of Nephrology, Shanghai Sixth People's Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, 200233, China.
Among the complications of diabetes, diabetic kidney disease (DKD) frequently emerges, typified by the detrimental effects on renal function, manifesting through inflammation, dysregulated lipid metabolism, and harm to podocytes. Existing research underscores the significance of the soluble form of C-X-C chemokine ligand 16 (CXCL16) within the context of renal impairments. However, whether CXCL16 is involved in the pathogenesis of DKD remains elusive.
View Article and Find Full Text PDFDeciphering phosphodiesterase-5 inhibitors from : computational models against erectile dysfunction.
In Silico Pharmacol
November 2024
Phyto-medicine and Computational Biology Lab, Department of Biochemistry, Adekunle Ajasin University, Akungba-Akoko, Ondo State Nigeria.
Unlabelled: Insufficient and inability to maintain erection in male for satisfactory sexual performance remains global challenge among couples. The identification of phosphodiesterase-5 (PDE-5) antagonist in the pathogenesis of erectile dysfunction has improved the search for therapeutic agents for the management of this sexual dysfunction. Here in, bioactive compounds from were virtually screened against PDE-5 using Schrodinger suite 2017-1 as computational tool.
View Article and Find Full Text PDFWant 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!