Synthesis and reduction reaction of novel triazole compounds in the solid-media condition by using microwave method

Some new triazole-3-one compounds have been synthesized and then reduction of carbonyl group in the molecule has been carried out to give a corresponding hydroxyl group which possesses asymmetric carbon atom in good yields, short reaction times and an eco-friendly approach in solvent-free condition by using microwave irradiation

Microwave assisted synthesize of new some benzimidazole derivatives and determination of protonation constant of these compounds in non-aqueous media

A series of 2-substituted benzimidazole derivatives have been synthesized via microwave mediated process. Different benzimidazole derivatives were titrated with tetrabutylammonium hydroxide in four non-aqueous solvents (isopropyl alcohol, N,N-dimethylformamide,tert-butyl alcohol and acetonitrile), using potentiometric method. The half neutralization potential values and the corresponding pKa values were determined for all cases

MICROWAVE-ASSISTED SYNTHESIS OF SOME 2-SUBSTITUTED QUINAZOLIN-4(3H)-ONE DERIVATIVES FROM IMINOESTER HYDROCHLORIDES

WOS: 000343615200009Herein, a method that involves a reaction of iminoester hydrochloride with methyl anthranilate via microwave assisted synthesis is reported. This efficient procedure provides pure products within few minutes. This method can be used as a general technique for synthesizing quinazoline derivatives

Synthesis and Urease Inhibition Study of Some New Quinazolinone Derivatives Bearing Triazole, Thiadiazole, and Piperazine Moiety

WOS: 000450023400011A new series of 2,3-disubstituted quinazolin-4(3H)-one derivatives bearing triazole and thiadiazole nucleus has been synthesized and then screened for their urease inhibition properties. All synthesized compounds showed outstanding urease inhibitory potentials with IC50 values ranging between 0.25 +/- 0.01 and 18.00 +/- 0.64 mu g/mL when compared with standard inhibitors thiourea (IC50 = 15.08 +/- 0.71 mu g/mL) and acetohydroxamic acid (IC50 = 21.05 +/- 0.96 mu g/mL). All new molecules were characterized by H-1 NMR, C-13 NMR, and MS.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [115Z885]; TUBITAKTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK)This work was supported by the Scientific and Technological Research Council of Turkey (TUBITAK) under the project number of 115Z885. the authors gratefully thank TUBITAK for financial support

Synthesis and characterisation of some coumarin-1,2,4-triazol-3-thioether hybrid molecules

WOS: 000396360600002A new series of N'-{[(4-methyl/phenyl-5-phenyl-4H-1,2,4-triazol-3-yl) thio] acetyl}-2-oxo-2H-chromene-3-carbohydrazides was synthesised via the reaction of 2-[(4-methyl/phenyl-5-phenyl-4H-1,2,4-triazol-3-yl) thio] acetohydrazides and 3-(1H-benzotriazol-1-ylcarbonyl)-2H-chromen-2- ones in good yields

Microwave Assisted Synthesis of Cournarins: A Review From 2007 to 2018

WOS: 000459402100001Background: Microwave heating has been shown to be an invaluable technology for medicinal chemistry and drug discovery applications. Recently, it has been used for heterocyclic synthesis increasingly. This review article shows a work on the synthesis of coumarin derivatives by microwave-assisted heating. Methods: Microwave-assisted heating has been used for the synthesis of coumarin derivatives. There are some useful methods to obtain coumarin derivatives. the Knoevenagel. condensation is the most prominent one with microwave heating. the other one is the microwave-assisted Vilsmeier-Haack reaction. Another one is microwave assisted convenient one-pot synthesis of coumarin derivatives via Pechmann condensation catalyzed by FeF3 under solvent-free conditions. in addition to these, Perkin condensation can also he used for the synthesis of coumarin derivatives under microwave heating conditions. Results: Coumarin derivatives have a pharmacological importance in drug discovery and dyes. Microwave irradiation is an effective method for the synthesis of coumarin derivatives and when compared to the conventional heating, it has many advantages. Conclusion: This review aimed to demonstrate the applications of microwave heating for the synthesis of coumarin derivatives from 2007 to 2018. It may be helpful to synthesize new coumarin derivatives as an alternative method that enables you to gain time and a new perspective

Microwave-Assisted Synthesis of Benzimidazoles and Their Derivatives From 1994 to 2016-A Review

WOS: 000410861300010Background: the use of microwave irradiation is an important development for the synthesis of benzimidazoles in the 21st century, and in recent years, microwave-assisted heterocyclic synthesis has gained significant attention in modern drug discovery studies. Benzimidazoles are an important group in the field of medicinal chemistry because of a wide range of biological activities. This review article provides a collection of studies on the synthesis of benzimidazole derivatives by microwave techniques over a twenty-one years period for an alternative to conventional heating. Methods: Microwave irradiation has been applied for the synthesis of benzimidazoles. the most used method for the preparation of benzimidazoles is condensation of o-diaminobenzene with carboxylic acids or derivatives. Results: Benzimidazoles have a seminal role in drug discovery and these derivatives show an excellent scaffold for the development of novel drugs, polymers, ligands and dys. Microwave heating is a useful technique for the synthesis of benzimidazole derivatives. When compared to the conventional heating methods, many advantages, such as reduction in reaction times, greater yield and purity provision, and less energy requirement, and creation of environmentally friendly conditions have been noted. Conclusion: This review aimed to demonstrate the applications of microwave for the synthesis of benzimidazole and their derivatives from 1994-2016. Microwave-assisted heterocyclic synthesis is a method that can be used to quickly explore and increase diversity in modern chemistry. in the light of the these studies, it could be argued that nearly all of the previously conventionally heated reactions could be performed using the microwave heating. We hope that this review will be helpful to synthesize new potential bioactive benzimidazole derivatives by using this effective method. Time is a very important dimension for researches people. If you save time, you can research much more. in this respect, the microwave technique helps researchers to make effective studies

SYNTHESIS AND STUDY OF ANTITUMOR ACTIVITY OF SOME NEW 2-(4-METHOXYBENZYL)-1H-BENZIMIDAZOLE DERIVATIVES BEARING TRIAZOLE, OXADIAZOLE AND ETHANOL MOIETY

WOS: 000381065300006A series of novel 1,2-disubstituted benzimidazole derivatives containing hydrazinecarbothioamide (7a-c), 1,2,4-triazole (8a-c) and 1,3,4-oxadiazole (5) moiety were synthesized starting from 2-(4-methoxybenzyl)-1H-benzimidazole. Then, the compounds 8a-c, 5 were converted to allcylated analogs (9a-c, 6) in the presence of K2CO3 and 2-bromoethanol. the structures of all the synthesized compounds were elucidated by H-1, C-13 NMR and mass spectroscopy. the newly synthesized compounds were tested on the five human cancer cells (breast (BT-20), melanoma (SK-Mel 128), prostate (DU-145), liver (SNU-398) andlung (A549)). the compound 7a had some degree of cytotoxicity against BT-20.Department of Scientific Research Project of Recep Tayyip Erdogan University [2014.102.02.03]We thank Department of Scientific Research Project of Recep Tayyip Erdogan University for financial assistance (Project no: 2014.102.02.03)

Synthesis and solvent-dependent photophysics of a novel fluorescent triazole-coumarin-based dye

WOS: 000508218100001Synthesis of a new coumarin-triazole-based dye and its photophysical parameters such as absorption, fluorescence emission, and fluorescence quantum yield were investigated. Studies have shown that the present dye has symmetry with a mirror image, especially in the ethanol solvent, with respect to the absorption and fluorescence spectra. As a result of the UV-vis and fluorescence spectroscopy techniques used, it was determined that absorption and emission spectra were shifted to the red with increasing solvent polarity. in addition, the spectral data of the synthesized compound exhibited that the stokes shifts are small, usually less than 50 nm, and the quantum yields are significantly high. in accordance with the results obtained, it can be stated that this novel dye synthesized here can offer an insight into application in sensor applications as analytical or biosensors, optoelectronic devices, and medicine industry.Recep Tayyip Erdogan University, Department of ChemistryResearch Fund of Recep Tayyip Erdogan University, Department of Chemistr

Synthesis, alpha-glucosidase inhibition and in silico studies of some 4-(5-fluoro-2-substituted-1H-benzimidazol-6-yl)morpholine derivatives

emirik, mustafa/0000-0001-9489-9093WOS: 000552631700004PubMed: 32563964In this study, a new series of 4-(5-fluoro-2-substituted-1H-benzimidazol-6-yl)morpholine derivatives has been synthesized and screened for their alpha-glucosidase inhibitory potential. All molecules showed a considerable alpha-glucosidase inhibitory potential with IC50 values ranging from 20.46 +/- 0.21 to 0.18 +/- 0.01 mu g/mL when compared with the acarbose (IC50 = 8.16 +/- 0.12 mu g/mL) as the standard. Compound 4 k having methoxy group on phenyl ring had the highest inhibitory effect with IC50 = 0.18 +/- 0.01 mu g/mL value among the examined compounds. Electron-donating groups such as methyl and methoxy on the phenyl ring played an important role in the inhibition. Also, the Lineweaver-Burk plots analysis displayed that the inhibition type of 4k was the competitive mode like acarbose as standard. in silico studies were also performed to explore the binding interaction of the most active compound