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Design, Synthesis and Microbiological Evaluation of Novel Compounds as Potential Staphylococcus aureus Phenylalanine tRNA Synthetase Inhibitors

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Last updated: 22 Jan 2023

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-

Tags

Organic chemistry

Abstract

As the resistance of Staphylococcus aureus to antibiotics represents a major threat to global health, anti-infectives with novel mechanisms must be developed. Novel compounds were generated as potential phenylalanine tRNA synthetase (PheRS) inhibitors based on the published homology model of S. aureus PheRS to aid the design process using Molecular Operating Environment (MOE) software. PheRS was selected as it is structurally unique enzyme among the aminoacyl-tRNA syntheases (aaRS), it is considerably different from human cytosolic and human mitochondrial aaRS and it is essential and conserved across bacterial species. The designed compounds were synthesized according to different clear schemes. The compounds were confirmed by 1H NMR, 13C NMR, HRMS and/or microanalysis, and they were microbiologically evaluated.

DOI

10.21608/ejchem.2018.4070.1357

Keywords

Staphylococcus aureus, Phenylalanine tRNA synthetase, Drug design, Benzimidazole, Indole, Adenine

Authors

First Name

Samar S.

Last Name

Elbaramawi

MiddleName

-

Affiliation

School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK, Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig P.C. 44519, Egypt

Email

-

City

-

Orcid

-

First Name

Casey

Last Name

Hughes

MiddleName

-

Affiliation

Department of Chemistry, University of Texas – Rio Grande Valley, 1201 W. University Drive, Edinburg, TX 78541, USA

Email

-

City

-

Orcid

-

First Name

Jennifer

Last Name

Richards

MiddleName

-

Affiliation

Specialist Antimicrobial Chemotherapy Unit, University Hospital of Wales, Heath Park, Cardiff CF14 4XW, UK

Email

-

City

-

Orcid

-

First Name

Arya

Last Name

Gupta

MiddleName

-

Affiliation

School of Molecular & Cellular Biology, Garstang Building, Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, UK

Email

-

City

-

Orcid

-

First Name

Samy M.

Last Name

Ibrahim

MiddleName

-

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig P.C. 44519, Egypt

Email

-

City

-

Orcid

-

First Name

El-Sayed M.

Last Name

Lashine

MiddleName

-

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig P.C. 44519, Egypt

Email

-

City

-

Orcid

-

First Name

Mohamed E.

Last Name

El-Sadek

MiddleName

-

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig P.C. 44519, Egypt

Email

-

City

-

Orcid

-

First Name

Alex J.

Last Name

O'Neill

MiddleName

-

Affiliation

School of Molecular & Cellular Biology, Garstang Building, Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, UK

Email

-

City

-

Orcid

-

First Name

Mandy

Last Name

Wootton

MiddleName

-

Affiliation

Specialist Antimicrobial Chemotherapy Unit, University Hospital of Wales, Heath Park, Cardiff CF14 4XW, UK

Email

-

City

-

Orcid

-

First Name

James M.

Last Name

Bullard

MiddleName

-

Affiliation

Department of Chemistry, University of Texas – Rio Grande Valley, 1201 W. University Drive, Edinburg, TX 78541, USA

Email

-

City

-

Orcid

-

First Name

Claire

Last Name

Simons

MiddleName

-

Affiliation

School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK

Email

-

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

2018-06-12

Publish Date

2018-12-01

Page Start

9

Page End

25

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 61_Issue Conference issue (14th Ibn Sina Arab Conference on Heterocyclic Chemistry and its Applications (ISACHC 2018), 30 March-2 April 2018, Hurgada, Egypt)._Pages 9-25.pdf

PDF . 1.4MB

Link

https://ejchem.journals.ekb.eg/article_9017.html

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https://ejchem.journals.ekb.eg/service?article_code=9017

Order

28

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