ManageChatDiscover
391403

Synthesis and Antimicrobial Screening of Novel 2-Thiopyrimidine Derivatives Bearing Pyrazole Moiety

Article

Last updated: 29 Mar 2025

OverviewSimilar Items

Subjects

-

Tags

Pharmaceutical Chemistry

Abstract

2-Thiouracil-5-carbonitrile derivatives 2a,b were used as starting material for synthesis of the chloropyrimidines 3a,b , and then reacted with thiourea to give the pyrimidine dithione derivatives 4a,b. The chloropyrimidines 3a,b were then methylated with methyl iodide to yield the methyl mercaptopyrimidines 5a,b. Following that , 4-mercapto-2-thiopyrimidine derivatives 6a,b were synthesized via a reaction between methyl mercaptopyrimidines 5a,b and thioura. Moreover, from 6a,b a series of thiopyrimidines derivatives 7a,b and 8a,b were synthesized. All compounds were screened against select microorganisms to assess their antimicrobial activity. Compounds 4b, 6a, and 8b showed the highest antibacterial activity among the synthesized derivatives . As a result, the three compounds were selected for a molecular docking study against the bacterial dihydropteroate synthase enzyme to which they revealed a good binding affinity.

DOI

10.21608/ejchem.2024.323611.10511

Keywords

Thiopyrimidine-5-carbonitrile, Antimicrobial, dihydropteroate synthase, Molecular docking

Authors

First Name

Ali J.

Last Name

Hekel

MiddleName

-

Affiliation

Pharmaceutical Chemistry Department, Faculty of pharmacy, Helwan University, Egypt

Email

ag706678@gmail.com

City

-

Orcid

-

First Name

Samir M.

Last Name

Awad

MiddleName

-

Affiliation

Pharmaceutical Organic Chemistry Department, Faculty of pharmacy, Helwan University, Egypt

Email

samirawad2000@yahoo.com

City

cairo

Orcid

0000-0001-7847-8301

First Name

Ola

Last Name

Nosseir

MiddleName

-

Affiliation

Pharmaceutical Chemistry Department, Faculty of pharmacy, Helwan University, Egypt

Email

ola.nosseir@pharm.helwan.edu.eg

City

-

Orcid

-

First Name

Mohamed F.

Last Name

El-Shehry

MiddleName

-

Affiliation

Pesticides Chemistry Department, National Research Centre, Dokki, Giza, 12622 Egypt

Email

moh_elshehry2000@yahoo.com

City

-

Orcid

-

First Name

Ahmed A.

Last Name

El-Rashedy

MiddleName

-

Affiliation

Natural and Microbial Products Department, National Research Center, Egypt

Email

ahmedelrashedy45@gmail.com

City

Giza

Orcid

0000-0003-3899-5376

First Name

Sherif F.

Last Name

Hammad

MiddleName

-

Affiliation

Pharmaceutical Chemistry Department, Faculty of pharmacy, Helwan University, Egypt , Pharm D Program, Egypt-Japan University of Science and Technology, New Borg-Arab City Alexandria 21934, Egypt

Email

sheriff.hammad@ejust.edu.eg

City

-

Orcid

-

Volume

68

Article Issue

5

Related Issue

54251

Issue Date

2025-05-01

Receive Date

2024-09-24

Publish Date

2025-05-01

Page Start

645

Page End

652

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 68_Issue 5_Pages 645-652.pdf

PDF . 1.1MB

Link

https://ejchem.journals.ekb.eg/article_391403.html

Detail API

http://journals.ekb.eg?_action=service&article_code=391403

Order

391,403

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

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

MainTitle

Synthesis and Antimicrobial Screening of Novel 2-Thiopyrimidine Derivatives Bearing Pyrazole Moiety

Details

Type

Article

Created At

29 Mar 2025