Synthesis, Characterization and Antimicrobial Activity of Some Novel Quinoline Derivatives Bearing Pyrazole and Pyridine Moieties
Amer, A., El-Eraky, W., Mahgoub, S. (2018). Synthesis, Characterization and Antimicrobial Activity of Some Novel Quinoline Derivatives Bearing Pyrazole and Pyridine Moieties. EKB Journal Management System, 61(Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt).), 1-8. doi: 10.21608/ejchem.2018.3941.1345
Atef Amer; W. I. El-Eraky; Sebaey Mahgoub. "Synthesis, Characterization and Antimicrobial Activity of Some Novel Quinoline Derivatives Bearing Pyrazole and Pyridine Moieties". EKB Journal Management System, 61, Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt)., 2018, 1-8. doi: 10.21608/ejchem.2018.3941.1345
Amer, A., El-Eraky, W., Mahgoub, S. (2018). 'Synthesis, Characterization and Antimicrobial Activity of Some Novel Quinoline Derivatives Bearing Pyrazole and Pyridine Moieties', EKB Journal Management System, 61(Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt).), pp. 1-8. doi: 10.21608/ejchem.2018.3941.1345
Amer, A., El-Eraky, W., Mahgoub, S. Synthesis, Characterization and Antimicrobial Activity of Some Novel Quinoline Derivatives Bearing Pyrazole and Pyridine Moieties. EKB Journal Management System, 2018; 61(Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt).): 1-8. doi: 10.21608/ejchem.2018.3941.1345

Synthesis, Characterization and Antimicrobial Activity of Some Novel Quinoline Derivatives Bearing Pyrazole and Pyridine Moieties

Egyptian Journal of Chemistry
Article 25, Volume 61, Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt)., November and December 2018, Page 1-8  XML PDF (636.84 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2018.3941.1345
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Authors
Atef Amer email 1; W. I. El-Eraky2; Sebaey Mahgoub3
1Department of Chemistry, Faculty of Science, Zagazig University, Egypt
2Department of Pharmacology, National Research Centre, Cairo, Egypt
3Research and Development, Unipharma, El-Obour City, Egypt
Abstract
In continuation of our interest in synthesis of novel quinoline derivatives with anticipated biological activity, we have synthesized new quinoline derivatives bearing pyrazole and pyridine moieties by formylation of quinoline hydrazones through the Vilsmeier-Haack reaction which is a common method for the synthesis of 4-formyl pyrazoles. Condensation of 2-hydrazinylquinoline 1 with 4-substituted acetophenone gave the corresponding hydrazones 2a–c which in turn underwent the Vilsmeier-Haack reaction in POCl3/DMF to furnish the corresponding 4-formyl pyrazole derivatives 3a–c. One-pot reaction of compounds 3a–c with malononitrile and thiophenol or ethyl mercaptan gave the 3,5-pyridinedicarbonitrile derivatives 11a–f. The synthesized derivatives were screened for their antimicrobial activities against Gram negative bacteria, Gram positive bacteria and fungi. Most of compounds showed excellent antimicrobial activities compared to the reference drugs. All the newly synthesized compounds have been characterized by means of elemental analyses, IR, 1H-NMR and MS.
Keywords
Quinoline; Vilsmeier-Haack reaction; 4-Formyl pyrazole; 3; 5-Pyridine dicarbonitrile; antimicrobial activity
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