735273-33-3Relevant academic research and scientific papers
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, 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.
System and method for preparing 6-mercapto polysubstituted pyridine derivative through three-component one-pot reaction
-
Paragraph 0121; 0122, (2017/12/28)
The invention discloses a system and method for preparing a 6-mercapto polysubstituted pyridine derivative through a three-component one-pot reaction, belonging to the technical field of organic synthesis. The preparation system for the 6-mercapto polysubstituted pyridine derivative comprises a raw material mixing device, a microwave reaction device, a suction filtration device, a washing device and a vacuum drying device which are sequentially arranged, wherein the microwave reaction device is used for a microwave heating reaction of raw materials in the raw material mixing device; the suction filtration device is used for suction filtration of a reaction product; the washing device and the vacuum drying device are used for washing and vacuum drying of a filter residue obtained after filtering, respectively. According to the invention, aromatic aldehydes, malononitrile and mercapto compounds are used as reaction materials, and the 6-mercapto polysubstituted pyridine derivative is prepared under the catalysis of an alkaline ionic liquid catalyst. The catalyst used in the invention is high in catalytic activity and low in usage amount and cyclic loss; and the prepared derivate has high yield and high purity.
A convenient Baker yeast accelerated, one-pot synthesis of pentasubstituted thiopyridines
Chavan, Anusaya S.,Kharat, Arun S.,Bhosle, Manisha R.,Mane, Ramrao A.
supporting information, p. 1777 - 1782 (2017/09/23)
Here we report a novel Baker yeast catalyzed one pot cyclocondensation, performed at room temperature in ethanol for obtaining high yields of polyfunctionalized pyridines, 2-amino-4-aryl-3,5-dicyano-6-phenylthiopyridines. The developed protocol obeys cert
Heterogeneous Cu(II)/l-His@Fe3O4 nanocatalyst: A novel, efficient and magnetically-recoverable catalyst for organic transformations in green solvents
Norouzi, Masoomeh,Ghorbani-Choghamarani, Arash,Nikoorazm, Mohsen
, p. 92387 - 92401 (2016/10/11)
A novel, efficient and green Cu(ii)/l-His@Fe3O4 catalyst has been applied successfully in the synthesis of heterocyclic compounds. The resulting catalyst was used in the synthesis of 2,3-dihydroquinazolin-4(1H)-ones, polyhydroquinolines and 2-amino-6-(arylthio)pyridine-3,5-dicarbonitriles as biologically interesting compounds. The present research is focused on investigation of recycling, reusability and stability of the catalyst in phase reactions. The Cu(ii)/l-His@Fe3O4 catalyst was used at least six times with comparable activities to that of fresh catalyst. The chemical composition and the structure of the catalyst were analysed by TGA/DTG, EDS, XRD, VSM, FT-IR and SEM.
A green catalytic preparation 2-amino-4-phenyl-6 - (phenyl-yl) - 3,5-di-cyano pyridine derivatives
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Paragraph 0036-0038, (2020/02/07)
The invention discloses a green catalytic method for preparing 2-amino-4-phenyl-6-(phenylthio)-3,5-dicyanopyridine derivatives, belonging to the field of organic chemical synthesis. The method comprises the following steps: reacting aromatic aldehyde, mal
Phosphotungstic acid catalyzed one-pot synthesis of 2-amino-3,5-dicarbonitrile-6-thio-pyridines in aqueous media
Su, Miao Shen,Ji, Xiao Jing,Zhao, Bing Bing,Tian, Meng,Ma, Jing Jun
, p. 1130 - 1134 (2016/01/12)
In this study, we report the one-pot synthesis of 2-amino-3,5-dicarbonitrile-6-thiopyridines with benzaldehyde, malononitrile, and thiophenol by using phosphotungstic acid as an efficient catalyst in aqueous media. This method has the advantages of easy s
Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists
Louvel, Julien,Guo, Dong,Soethoudt, Marjolein,Mocking, Tamara A.M.,Lenselink, Eelke B.,Mulder-Krieger, Thea,Heitman, Laura H.,Ijzerman, Adriaan P.
, p. 681 - 691 (2015/08/03)
Abstract We report the synthesis and biological evaluation of new derivatives of Capadenoson, a former drug candidate that was previously advanced to phase IIa clinical trials. 19 of the 20 ligands show an affinity below 100 nM at the human adenosine A1 receptor (hA1AR) and display a wide range of residence times at this target (from approx. 5 min (compound 10) up to 132 min (compound 5)). Structure-affinity and structure-kinetics relationships were established, and computational studies of a homology model of the hA1AR revealed crucial interactions for both the affinity and dissociation kinetics of this family of ligands. These results were also combined with global metrics (Ligand Efficiency, cLogP), showing the importance of binding kinetics as an additional way to better select a drug candidate amongst seemingly similar leads.
Sodium chloride: A proficient additive for the synthesis of pyridine derivatives in aqueous medium
Gujar, Jitendra B.,Chaudhari, Mahendra A.,Kawade, Deepak S.,Shingare, Murlidhar S.
, p. 6939 - 6942 (2015/01/08)
A facile and convenient synthesis of substituted pyridine derivatives catalysed by NaCl in the presence aqueous media under reflux and ultrasound irradiation has been developed via a one-pot multicomponent reaction, in which four new bonds were formed. Pa
