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Hit Identification Against Candida Albicans: Design, Synthesis, Molecular Docking and Biological Evaluation of Hybrid Styryl-Quinoxaline Based Analogues.

Article

Last updated: 01 Jan 2025

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Abstract

The occurrence of invasive fungal infections (IFIs) and the incidence of resistant fungal pathogens have increased dramatically, leading to high morbidity and mortality especially with immune-compromised patients. Owing to their multifunctional pharmacological profiles, quinoxalines attract widespread attention being a part of several biologically and technologically relevant compounds. Herein, we report the design, synthesis, structural characterization, and biological screening of a series of new quinoxaline-based scaffolds. The antimicrobial activities of the synthesized compounds were assessed against a panel of bacterial species as well as representative fungi. Interestingly, N-(3-chlorophenyl)-2-(3-(2-hydroxystyryl)quinoxalin-2-yl) hydrazinecarboxamide (3a) displayed significant antifungal activity against Candida albicans (MIC50 ≤0.25 µg/mL) compared to that of the reference drug fluconazole (MIC50 =0.125 µg/mL). Molecular docking studies showed that the potency of our compounds could be attributed to the inhibition of fungal squalene epoxidase enzyme. Additionally, all synthesized compounds were almost neither toxic to human embryonic kidney cells (CC50 >32.0 µg/mL) nor to human red blood cells (HC10 >32.0 µg/mL). The above finding results suggested that compounds 3a is a promising lead compound that merits further optimization and development as antifungal candidate.

DOI

10.21608/ejchem.2023.205360.7850

Keywords

Fungal infection, Candida albicans, quinoxaline, styryl, Squalene epoxidase

Authors

First Name

Aliya

Last Name

El Newahie

MiddleName

Mohamed shaker

Affiliation

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, October University for Modern Science and Arts (MSA), Cairo, 12611, Egypt

Email

anewahie@msa.edu.eg

City

Cairo

Orcid

ORCID: 0000-0001-7061-5869

First Name

Maiy Y.

Last Name

Jaballah

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Abbassia, Cairo, 11566, Egypt

Email

mai.youssef@pharma.asu.edu.eg

City

Cairo

Orcid

0000-0002-8221-8710.

First Name

Mohamed

Last Name

Alaraby

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Cairo, 12611, Egypt

Email

msalem@ualberta.ca

City

Cairo

Orcid

0000-0002-4369-7077

First Name

Mohamed

Last Name

elbadawy

MiddleName

-

Affiliation

Department of Microbiology and Immunology, Faculty of Pharmacy, University of Sadat City, Sadat city, Menoufia, 32897,Egypt

Email

mohamed.elbadawy@fop.usc.edu.eg

City

Cairo

Orcid

0000-0002-5896-3067

First Name

Rabah

Last Name

Serya

MiddleName

Ahmed

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Abbassia, Cairo, 11566, Egyp

Email

rabah@pharma.asu.edu.eg

City

Cairo

Orcid

0000-0002-1349-7269

First Name

Aliaa

Last Name

Kamal

MiddleName

mohamed

Affiliation

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, October University for Modern Science and Arts (MSA), Cairo, 12611, Egypt

Email

alkamal@msa.edu.eg

City

Cairo

Orcid

0000-0002-4897-2795

First Name

Khaled

Last Name

Abouzid

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Abbassia, Cairo, 11566, Egypt

Email

khaled.abouzid@pharma.asu.edu.eg

City

-

Orcid

0000-0001-9851-5624

Volume

66

Article Issue

13

Related Issue

43707

Issue Date

2023-12-01

Receive Date

2023-04-11

Publish Date

2023-12-01

Page Start

1,295

Page End

1,308

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 66_Issue 13_Pages 1295-1308.pdf

PDF . 1.8MB

Link

https://ejchem.journals.ekb.eg/article_300215.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=300215

Order

300,215

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

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

MainTitle

Hit Identification Against Candida Albicans: Design, Synthesis, Molecular Docking and Biological Evaluation of Hybrid Styryl-Quinoxaline Based Analogues.

Details

Type

Article

Created At

30 Dec 2024