Beta
9014

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

Article

Last updated: 22 Jan 2023

Subjects

-

Tags

Organic chemistry

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

First Name

Atef

Last Name

Amer

MiddleName

-

Affiliation

Department of Chemistry, Faculty of Science, Zagazig University, Egypt

Email

atefamer55@yahoo.com

City

-

Orcid

-

First Name

W. I.

Last Name

El-Eraky

MiddleName

-

Affiliation

Department of Pharmacology, National Research Centre, Cairo, Egypt

Email

-

City

-

Orcid

-

First Name

Sebaey

Last Name

Mahgoub

MiddleName

-

Affiliation

Research and Development, Unipharma, El-Obour City, Egypt

Email

dr_semahgoub@yahoo.com

City

-

Orcid

-

Volume

61

Article Issue

Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt).

Related Issue

2068

Issue Date

2018-12-01

Receive Date

2018-05-25

Publish Date

2018-12-01

Page Start

1

Page End

8

Print ISSN

0449-2285

Online ISSN

2357-0245

Link

https://ejchem.journals.ekb.eg/article_9014.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=9014

Order

25

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

https://ejchem.journals.ekb.eg/

MainTitle

-

Details

Type

Article

Created At

22 Jan 2023