Microwave-Assisted Synthesis and Cytotoxicity Evaluation of Some Novel Pyrazole Containing Imidiazole, Pyrazole, Oxazole, Thiadiazole and Benzochromene derivatives

Hafez, Hend N.

doi:10.21608/ejchem.2017.1824.1151

Cited by 8 publications

(9 citation statements)

References 29 publications

(33 reference statements)

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“…Dyes have been used as natural and synthetic products for a variety of applications, such as inkjet printing, plastics, textile coloration, adhesives, beverages, ceramics, photography, cosmetics, foodstuff, optoelectronics, coatings, sensors, xerography, constructions and biomedical applications [1][2][3][4][5][6][7][8][9][10][11][12][13][14]. Heteroaromatic compounds have been used in various fields of life sciences and technology [15][16][17][18][19][20][21]. Numerous of heterocyclic dyes are now commercialized to produce a full range of dyestuffs especially for textile coloration.…”

Section: Introductionmentioning

confidence: 99%

A review on synthesis of nitrogen-containing heterocyclic dyes for textile fibers - Part 2: Fused heterocycles

Khattab

Rehan

2018

Egypt. J. Chem.

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I MPORTANCE of heterocyclic dyes has recently increased due to their deep shades, high tentorial strength, excellent colorfastness and brightness compared to azobenzene analogous. Development of novel synthetic approaches for fused heterocyclic dyes has remained a highly interesting but challenging proposition. An overview of the application of nitrogen-containing fused heterocyclic dyestuffs for textile coloration is presented. In this review, we provide details outlining the synthesis of recently prepared fused nitrogen-containing heterocyclic dyestuffs and their dyeing efficiency on textile fibers.

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Section: Introductionmentioning

confidence: 99%

A review on synthesis of nitrogen-containing heterocyclic dyes for textile fibers - Part 2: Fused heterocycles

Khattab

Rehan

2018

Egypt. J. Chem.

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“…Mass spectroscopy or microanalysis was not conducted for the structures of the prepared compounds owing to the instability (Scheme 1). 5-(2-(1H-benzimidazol-1-yl)ethyl)-1,3,4thiadiazol-2-amine (9) was achieved by the reaction of a methanolic solution of 3-(1H-benzimidazol-1-yl)propane hydrazide (5a) with KSCN in acidic solution through a nucleophilic addition reaction [24,25]. The acidic condition afforded the cyclization of the 1,3,4-thiadiazole ring.…”

Section: Chemistrymentioning

confidence: 99%

Design, synthesis and microbiological evaluation of novel compounds as potential Staphylococcus aureus phenylalanine tRNA synthetase inhibitors

et al. 2018

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less than 90% of S. aureus strains are resistant to most penicillin derivatives [2] and ordinary antimicrobial agents like drugs from the family of aminoglycosides, macrolides, chloramphenicols, tetracyclines and fluoroquinolones so known as multidrug resistant Staphylococcus aureus [3]. Increased resistance of MRSA to anti-infective drugs is a threat to global health; so anti-infectives with novel mechanisms must be developed. Our potential target in the drug development for the treatment of MRSA infections is phenylalanine tRNA synthetase which is considered as the most complex and large enzyme of aminoacyl-tRNA synthetases (aaRSs). Aminoacyl-tRNA synthetases (aaRSs) (also A S THE RESISTANCE of Staphylococcus aureus to antibiotics represents a major threat to global health, anti-infectives with novel mechanisms must be developed. Novel compounds were generated as potential phenylalanine tRNA synthetase (PheRS) inhibitors based on the published homology model of S. aureus PheRS to aid the design process using Molecular Operating Environment (MOE) software. PheRS was selected as it is structurally unique enzyme among the aminoacyl-tRNA synthetases (aaRS), it is considerably different from human cytosolic and human mitochondrial aaRS and it is essential and conserved across bacterial species. The designed compounds were synthesized according to different clear schemes. The compounds were confirmed by 1 H NMR, 13 C NMR, HRMS and/or microanalysis, and they were microbiologically evaluated.

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“…In the present work, we employed several computational approaches for design of novel Rab23 inhibitors. The chromene derivatives are considered as the key structural compounds for many drugs having a broad spectrum of in medicinal and pharmaceutical chemistry, because of their multiplicity uses in drug industry [2], [3]. Additionally, the chromene nucleus is an important pharmacophore in many biologically active compounds [4], [5].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and Insilico molecular docking studies of novel chromene derivatives as Rab23 inhibitors

El‐Maghraby

Abdelmonsef

2019

Egypt. J. Chem.

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T HE Rab23 protein overexpression has a well-validated role in variety of human cancers. Therefore, the present research aimed to identify new Rab23 protein inhibitor candidates using computational based drug design methodology. A novel series of chromeno[2,3-b] pyridine derivatives has been synthesized by the cyclocondensation of 2-amino-3-cyano-4H-chromenes with cyclohexanone and cyclopentanone in ethanolic piperidine solution. The 2-amino-4H-chromenes were obtained using one pot multicomponent condensation of resorcinol, malononitrile and aromatic aldehydes in the presence in ethanolic piperidine solution. All newly synthetic compounds were characterized by spectral analysis IR, NMR and MS and elemental analysis techniques. The best binding modes of chromene derivatives were evaluated via molecular docking studies and binding energy calculations, using PyRx tool. The study has shown that the pyran and pyridine moieties interact favorably with the binding site of target protein, providing the mechanism of action against human sapiens Rab23 protein.

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Microwave-Assisted Synthesis and Cytotoxicity Evaluation of Some Novel Pyrazole Containing Imidiazole, Pyrazole, Oxazole, Thiadiazole and Benzochromene derivatives

Abstract: ) has excellent cytotoxic agents against the three tumor cell lines, which is more potent than the activity of doxorubicin.

Cited by 8 publications

References 29 publications

A review on synthesis of nitrogen-containing heterocyclic dyes for textile fibers - Part 2: Fused heterocycles

A review on synthesis of nitrogen-containing heterocyclic dyes for textile fibers - Part 2: Fused heterocycles

Design, synthesis and microbiological evaluation of novel compounds as potential Staphylococcus aureus phenylalanine tRNA synthetase inhibitors

Synthesis, characterization and Insilico molecular docking studies of novel chromene derivatives as Rab23 inhibitors

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