Synthesis, reaction, antimicrobial, and docking study of new chalcones incorporating isoquinoline moiety

Mukhtar, Shorouk S.; Saleh, Fatma M.; Hassaneen, Hamdi M.; Hafez, T. S.; Hassan, Ashraf S.; Morsy, Nesrin M.; Teleb, Mohamed A. Mohamed

doi:10.1080/00397911.2022.2119415

Cited by 2 publications

(1 citation statement)

References 43 publications

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“…Based on the above-mentioned information about bioactive pyrazole compounds, diseases-related complications, and interferences of the diseases in addition to a continuation of our program for the exploration of bioactive products [16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31], accordingly, we aim in this study to (i) synthesize three series of pyrazole-based derivatives 7a-c, 9a-c, and 11a-c. (ii) Estimate the biological activities of pyrazole-based products 7a-c, 9a-c, and 11a-c as antioxidant, anti-diabetic, anti-Alzheimer, and antiarthritic. (iii) Perform the in silico analysis including physicochemical, drug-likeness, and toxicity properties of the biologically potent products.…”

Section: Figurementioning

confidence: 99%

Synthesis, In Vitro Biological Investigation, and In Silico Analysis of Pyrazole-Based Derivatives as Multi-target Agents

Hassan

Aboulthana

2023

Egypt. J. Chem.

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The diseases-related complications and causes are threaded. Accordingly, the preparation of one drug with multiple targets is very pressing. In this context, the three series of pyrazole-based derivatives 7a-c, 9a-c, and 11a-c were designed and synthesized by using 5-amino-pyrazoles 3a-c as starting materials. The structures of various products 7a-c, 9a-c, and 11a-c were characterized by using various devices (elemental analysis and spectral tools). The biological activities of pyrazolebased products 7a-c, 9a-c, and 11a-c were estimated as antioxidant, anti-diabetic, anti-Alzheimer, and anti-arthritic. The estimation results showed that the two products 7c and 11a displayed powerful biological activities. In silico analysis (physicochemical, drug-likeness, and toxicity properties) of the two products 7c and 11a was performed. This research could be valuable for the exploration of one drug with multiple targets.

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Section: Figurementioning

confidence: 99%

Synthesis, In Vitro Biological Investigation, and In Silico Analysis of Pyrazole-Based Derivatives as Multi-target Agents

Hassan

Aboulthana

2023

Egypt. J. Chem.

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Advances in the Synthesis of Heterocycles with Two and Three Heteroatoms using Hydrazonoyl Halides

Yamaletdinova,

Gataullin

2024

Helvetica Chimica Acta

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The review covers the results of studies published in the literature on the use of hydrazonoyl halides in the synthesis of five‐ (pyrazoles, thiazoles, triazoles, oxa‐ and thiadiazoles), six‐ (oxa‐ and thiadiazines, indazoles, pyridazines, pyrazines, tetrazines) or seven‐membered (benzotriazepine) heterocycles. In the formation of these heterocycles, the main intermediate stage of the reaction is the in situ generation of nitrilimine, which enters into a cycloaddition reaction with substituted acetylenes (including in situ generated benzynes, naphthynes), allenes, activated olefins, anthranilic acid derivatives, organosulfur compounds (mercaptoaldehydes, mercaptocarboxylic acids ) or with fused heterocycles. Examples are given of the formation of heterocycles by replacing the halogen atom from a hydrazonoyl halide molecule with a nucleophilic group, followed by exhaustive intramolecular cyclization into the target compound. There are discussions of reactions in which the cycloaddition of the nitrilimine to the in situ synthesized Knoevenagel condensation product (from CH‐acid compounds, such as di‐ and monocarbonyl compounds, dinitrile malonic acid) occurs, leading to spiro‐linked or conventional pyrazoles. Some syntheses of biologically active representatives are shown.

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Synthesis, reaction, antimicrobial, and docking study of new chalcones incorporating isoquinoline moiety

Cited by 2 publications

References 43 publications

Synthesis, In Vitro Biological Investigation, and In Silico Analysis of Pyrazole-Based Derivatives as Multi-target Agents

Synthesis, In Vitro Biological Investigation, and In Silico Analysis of Pyrazole-Based Derivatives as Multi-target Agents

Advances in the Synthesis of Heterocycles with Two and Three Heteroatoms using Hydrazonoyl Halides

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