79359-40-3Relevant academic research and scientific papers
Discovery of Highly Potent Adenosine A1Receptor Agonists: Targeting Positron Emission Tomography Probes
Bakhoda, Abolghasem,Eisenberg, Seth M.,Fowler, Joanna S.,Gao, Zhan-Guo,Guo, Min,Hooker, Jacob M.,Jacobson, Kenneth A.,Javdan, Cameron,Kang, Yeona,Kelleher, Andrew C.,Kim, Sung Won,Li, Yang,O'Conor, Kelly A.,Ramsey, Joseph M.,Rice, Kenner C.,Volkow, Nora D.,Yan, Xuefeng
, (2021/09/27)
Adenosine receptor (AR) radiotracers for positron emission tomography (PET) have provided knowledge on the in vivo biodistribution of ARs in the central nervous system (CNS), which is of therapeutic interest for various neuropsychiatric disorders. Additio
Synthesis, in vitro and in silico screening of 2-amino-4-aryl-6-(phenylthio) pyridine-3,5-dicarbonitriles as novel α-glucosidase inhibitors
Ali, Muhammad,Faramarzi, Mohammad Ali,Jabbar, Abdul,Khan, Khalid Mohammed,Larijani, Bagher,Mahdavi, Mohammad,Perveen, Shahnaz,Salar, Uzma,Shamim, Shahbaz,Taha, Muhammad
, (2020/05/16)
Inhibition of α-glucosidase enzyme is of prime importance for the treatment of diabetes mellitus (DM). Apart of many organic scaffolds, pyridine based compounds have previously been reported for wide range of bioactivities. The current study reports a series of pyridine based synthetic analogues for their α-glucosidase inhibitory potential assessed by in vitro, kinetics and in silico studies. For this purpose, 2-amino-4-aryl-6-(phenylthio)pyridine-3,5-dicarbonitriles 1–28 were synthesized and subjected to in vitro screening. Several analogs, including 1–3, 7, 9, 11–14, and 16 showed many folds increased inhibitory potential in comparison to the standard acarbose (IC50 = 750 ± 10 μM). Interestingly, compound 7 (IC50 = 55.6 ± 0.3 μM) exhibited thirteen-folds greater inhibition strength than the standard acarbose. Kinetic studies on most potent molecule 7 revealed a competitive type inhibitory mechanism. In silico studies have been performed to examine the binding mode of ligand (compound 7) with the active site residues of α-glucosidase enzyme.
Natural dolomitic limestone-catalyzed synthesis of benzimidazoles, dihydropyrimidinones, and highly substituted pyridines under ultrasound irradiation
Godugu, Kumar,Gundala, Trivikram Reddy,Mohinuddin Pinjari, Mohammad Khaja,Reddy Nallagondu, Chinna Gangi,Sanapareddy, Lakshmi Reddy,Sri Yadala, Venkata Divya
supporting information, p. 1881 - 1900 (2020/10/02)
Natural dolomitic limestone (NDL) is employed as a heterogeneous green catalyst for the synthesis of medicinally valuable benzimidazoles, dihydropyrimidinones, and highly functionalized pyridines via C–N, C–C, and C–S bond formations in a mixture of ethan
Application of novel and reusable Fe3O4@CoII(macrocyclic Schiff base ligand) for multicomponent reactions of highly substituted thiopyridine and 4H-chromene derivatives
Ebrahimiasl, Hakimeh,Azarifar, Davood,Rakhtshah, Jamshid,Keypour, Hassan,Mahmoudabadi, Masoumeh
, (2020/06/08)
In this research study we designed and synthesized CoII(macrocyclic Schiff base ligand containing 1,4-diazepane) immobilized on Fe3O4 nanoparticles as a novel, recyclable, and heterogeneous catalyst. The nanomaterial was f
WEB (water extract of banana): An efficient natural base for one-pot multi-component synthesis of 2-amino-3,5-dicarbonitrile-6-thio-pyridines
Allahi, Alireza,Akhlaghinia, Batool
, p. 328 - 336 (2020/10/22)
One-pot multi-component synthesis of 2-amino-3,5-dicarbonitrile-6-thio-pyridines derivatives using WEB (water extract of banana peels ash) as a green catalyst is described. A variety of aromatic aldehydes (with electron-donating and electron-withdrawing groups) in conjunction with aromatic and aliphatic thiols are known to tolerate this reaction condition using WEB. The reaction has simple work up procedure without using toxic solvents.
Synthesis, Reactions and Antitumor Activity of Certain 1,3-diphenylpyrazole-4-carboxaldehyde Derivatives
Amer, Atef M.,Ramses, Neveen,Mahgoub, Sebaey
, p. 51 - 65 (2019/03/28)
IN activity continuation especially of our the interest antitumor in synthesis activity.In of novel this paper heterocycles we have with discussed anticipat
Unique role of 2-hydroxyethylammonium acetate as an ionic liquid in the synthesis of Fe3O4 magnetic nanoparticles and preparation of pyridine derivatives in the presence of a new magnetically recyclable heterogeneous catalyst
Sobhani, Sara,Nasseri, Fatemeh,Zarifi, Farzaneh
, p. 2721 - 2732 (2018/10/31)
Abstract: In this paper, 2-hydroxyethylammonium acetate (2-HEAA) was used as the first functionalized ionic liquid for the facile, economical and environmentally friendly synthesis of Fe3O4 nanoparticles by a co-precipitation method. The synthesized Fe3O4 nanoparticles were used as solid material for supporting 2-HEAA (Fe3O4-2-HEAA). The newly prepared Fe3O4-2-HEAA was characterized by TEM, XRD, FT-IR, TGA and elemental analysis and successfully applied as a magnetically recyclable heterogeneous catalyst for the efficient one-pot, three-component synthesis of 2-amino-3,5-dicarbonitrile-6-thio-pyridines. The catalyst was easily separated by an external magnet and reused at least five times without significant degradation in the activity.
Method for synthesizing polysubstituted pyridine compounds at room temperature
-
Paragraph 0026; 0027; 0035; 0043, (2018/04/02)
The invention discloses a method for synthesizing polysubstituted pyridine compounds at the room temperature. The method is technically characterized in that ethanediamine/trinitromethane eutectoid isadopted as a catalyst, an ethanol aqueous solution is t
Polysubstituted pyridine derivative and preparation method and application thereof
-
Paragraph 0016; 0017; 0018; 0020; 0021, (2018/11/22)
The invention discloses a polysubstituted pyridine derivative and a preparation method and the application thereof. The polysubstituted pyridine derivative adopts a structural formula 5. The preparation method comprises the following steps: in an organic
Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases
Meibom, Daniel,Albrecht-Küpper, Barbara,Diedrichs, Nicole,Hübsch, Walter,Kast, Raimund,Kr?mer, Thomas,Krenz, Ursula,Lerchen, Hans-Georg,Mittendorf, Joachim,Nell, Peter G.,Süssmeier, Frank,Vakalopoulos, Alexandros,Zimmermann, Katja
supporting information, p. 728 - 737 (2017/05/26)
Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine A1 receptors (A1Rs) has been shown to inhibit myocardial pathologies associated with ischemia and reperfusion injury, suggesting several options for new cardiovascular therapies. When full A1R agonists are used, the desired protective and regenerative cardiovascular effects are usually overshadowed by unintended pharmacological effects such as induction of bradycardia, atrioventricular (AV) blocks, and sedation. These unwanted effects can be overcome by using partial A1R agonists. Starting from previously reported capadenoson we evaluated options to tailor A1R agonists to a specific partiality range, thereby optimizing the therapeutic window. This led to the identification of the potent and selective agonist neladenoson, which shows the desired partial response on the A1R, resulting in cardioprotection without sedative effects or cardiac AV blocks. To circumvent solubility and formulation issues for neladenoson, a prodrug approach was pursued. The dipeptide ester neladenoson bialanate hydrochloride showed significantly improved solubility and exposure after oral administration. Neladenoson bialanate hydrochloride is currently being evaluated in clinical trials for the treatment of heart failure.
