Subjects
-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.
DOI
10.21608/ejchem.2018.3941.1345
Keywords
Quinoline, Vilsmeier-Haack reaction, 4-Formyl pyrazole, 3, 5-Pyridine dicarbonitrile, antimicrobial activity
Authors
MiddleName
-Affiliation
Department of Chemistry, Faculty of Science, Zagazig University, Egypt
Email
atefamer55@yahoo.com
City
-Orcid
-MiddleName
-Affiliation
Department of Pharmacology, National Research Centre, Cairo, Egypt
Email
-City
-Orcid
-MiddleName
-Affiliation
Research and Development, Unipharma, El-Obour City, Egypt
Email
dr_semahgoub@yahoo.com
City
-Orcid
-Article Issue
Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt).
Link
https://ejchem.journals.ekb.eg/article_9014.html
Detail API
https://ejchem.journals.ekb.eg/service?article_code=9014
Publication Title
Egyptian Journal of Chemistry
Publication Link
https://ejchem.journals.ekb.eg/
MainTitle
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