Aryl sulfonamido tetralins based on lead compound 2a were synthesized and evaluated for Kv1.5 inhibitory activity. Several compounds having IC(50) values less then 0.1 microM were identified. Kv1.5 inhibitors have the potential to be atrium-selective agents for the treatment of atrial fibrillation.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2009.04.002 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Design and Synthesis of Novel 2-Acetamido, 6-Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors - In vitro Evaluation of their Antiproliferative Activity.
ChemMedChem
November 2023
Institute of Chemical Biology, National Hellenic Research Foundation, Vas. Constantinou Ave. 48, 11635, Athens, Greece.
The oncogenic BRAFV600E kinase leads to abnormal activation of the MAPK signaling pathway and thus, uncontrolled cellular proliferation and cancer development. Based on our previous virtual screening studies which issued 2-acetamido-1,3 benzothiazole-6-carboxamide scaffold as active pharmacophore displaying selectivity against the mutated BRAF, eleven new substituted benzothiazole derivatives were designed and synthesized by coupling of 2-acetamidobenzo[d]thiazole-6-carboxylic acid with the appropriate amines in an effort to provide even more efficient inhibitors and tackle drug resistance often developed during cancer treatment. All derived compounds bore the benzothiazole scaffold substituted at position-2 by an acetamido moiety and at position-6 by a carboxamide functionality, the NH moiety of which was further linked through an alkylene linker to a sulfonamido (or amino) aryl (or alkyl) functionality or a phenylene linker to a sulfonamido aromatic (or non-aromatic) terminal pharmacophore in the order -C H -NHSO -R or reversely -C H -SO N(H)-R.
View Article and Find Full Text PDF1,2,3-Triazolo[4,5-b]aminoquinolines: Design, synthesis, structure, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity, and molecular docking of novel modified tacrines.
Bioorg Chem
October 2023
Núcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil. Electronic address:
An efficient [4 + 2] cyclization protocol to synthesize a series of twelve examples of 1,2,3-triazolo[4,5-b]aminoquinolines (5) as novel structurally modified tacrines was obtained by reacting readily accessible precursors (i.e., 3-alky(aryl)-5-amino-1,2,3-triazole-4-carbonitriles (3)) and selected cycloalkanones (4) of five-, six-, and seven-membered rings.
View Article and Find Full Text PDFConformationally Restricted Glycoconjugates Derived from Arylsulfonamides and Coumarins: New Families of Tumour-Associated Carbonic Anhydrase Inhibitors.
Int J Mol Sci
May 2023
Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Apartado 1203, E-41071 Seville, Spain.
The involvement of carbonic anhydrases (CAs) in a myriad of biological events makes the development of new inhibitors of these metalloenzymes a hot topic in current Medicinal Chemistry. In particular, CA IX and XII are membrane-bound enzymes, responsible for tumour survival and chemoresistance. Herein, a bicyclic carbohydrate-based hydrophilic tail (imidazolidine-2-thione) has been appended to a CA-targeting pharmacophore (arylsulfonamide, coumarin) with the aim of studying the influence of the conformational restriction of the tail on the CA inhibition.
View Article and Find Full Text PDFPhotoredox Catalysis for the Synthesis of N-CF H Compounds Using 1-((N-(difluoromethyl)-4-methylphenyl)-sulfonamido)pyridin-1-ium Trifluoromethanesulfonate.
Angew Chem Int Ed Engl
July 2023
Loker Hydrocarbon Research Institute, Department of Chemistry, University of Southern California, 837 Bloom Walk, 90089-1661, Los Angeles, CA, USA.
N-(difluoromethyl)amino (-NCF H) compounds are of great interest given their unique and underexplored physiochemical properties. The lack of structural diversity in NCF H compounds is likely due in part to the shortage of protocols for efficient installation. Presented herein is a new shelf-stable pyridinium reagent that enables the direct installation of the N-(difluoromethyl)sulfonamide moiety [N(Ts)CF H)] onto (hetero)arenes and alkenes for the diversification of aryl and alkyl NCF H compounds.
View Article and Find Full Text PDFOrganophotoredox-Catalyzed Cross-Dehydrogenative Sulfonamidation of Indoles and Other Heterocycles.
J Org Chem
July 2023
Department of Chemistry and Chemical Biology, Indian Institute of Technology (ISM), Dhanbad, Jharkhand 826004, India.
The visible light-triggered regioselective synthesis of 2-sulfonamidoindoles and other 2-sulfonamido heteroarenes is accomplished by the oxidative cross-dehydrogenative coupling of indoles (heteroarenes) with di--toluenesulfonamide or -aryl--toluenesulfonamides. The reaction was catalyzed by eosin-Y through a photoredox route. Detailed mechanistic studies based on control reactions, cyclic voltammetry, and fluorescence quenching have been reported for the elucidation of the mechanistic cycle and revealed that a nitrogen-centered radical is generated, followed by regioselective addition to the heteroarene.
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!