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64183

SYNTHESIS OF NEW 4(3H)-QUINAZOLINONE DERIVATIVES OF POTENTIAL ANTIMICROBIAL ACTIVITY

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Last updated: 25 Dec 2024

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Abstract

A new series of quinazoline-4(3H)-one derivatives containing hydrazone, thiosemicarbazide, pyrazole moiety and 1,2,4triazolo[4,3-a]quinazolin-5-(4H)-one derivatives, were prepared in order to study the effect of such combinations on the expected antimicrobial activity.  Synthesis of target compounds (3-8) has been achieved through an interaction of the starting 2a or 2b with different alkyl or aryl isothiocyanate. Condensation of 2a or 2b with various aromatic aldehydes or ketones afforded the corresponding hydrazones 9-12. 1-(4-Pyridinyl)-1,2-dihydro-4phenyl(allyl)-1,2,4-triazolo[4,3-a]quinazolin-5-(4H)-one deriva tives 13, 14 have been synthesized through reflux of compound 9 or 10 in glacial acetic acid.  On the other hand, 1-(3-substituted-3,4dihydro-4-quinazolinon-2-yl)-3-(4-chlorophenyl) pyrazole-4-carbaldehyde 15 or 16 has also been synthesized through interaction of compounds 11 or 12 with Vilsmeier-Haack reagent1. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their in vitro antibacterial and antifungal activities. The tested compounds showed moderate antibacterial activity and weak or no antifungal activity.

DOI

10.21608/bfsa.2007.64183

Authors

First Name

Awwad

Last Name

Radwan

MiddleName

A.

Affiliation

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71527, Egypt

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First Name

Salah

Last Name

Ali

MiddleName

G.

Affiliation

Department of Botany and Microbiology, Faculty of Science, Al-Azhar University, 71524 Assiut, Egypt

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Volume

30

Article Issue

2

Related Issue

9610

Issue Date

2007-12-01

Receive Date

2007-10-06

Publish Date

2007-12-31

Page Start

181

Page End

192

Print ISSN

1110-0052

Online ISSN

3009-7703

Link

https://bpsa.journals.ekb.eg/article_64183.html

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https://bpsa.journals.ekb.eg/service?article_code=64183

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7

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Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

SYNTHESIS OF NEW 4(3H)-QUINAZOLINONE DERIVATIVES OF POTENTIAL ANTIMICROBIAL ACTIVITY

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Article

Created At

22 Jan 2023