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300922

SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING

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Last updated: 04 Jan 2025

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Abstract

Since ancient times, several heterocyclic scaffolds have been recognized as possessing a wide spectrum of anti-infectious pharmacological properties. The present work aimed to synthesize and to perform antibacterial screening of some novel heterocyclic derivatives of thiadiazinyl β-lactam and thiazolidin-4-one. Cyclization of thiosemicarbazide with cyclohexanone and substituted aromatic aldehydes leads to the formation of Schiff bases, which form thiazolidinone derivatives upon reaction with thioglycolic acid in the presence of a catalytic amount of ZnCl2. Lactam derivatives were synthesized by the cyclization of Schiff bases with chloroacetyl chloride in presence of triethyl amine. The synthesized derivatives 2a (MIC 25 µg/ml), and 3f (MIC 25 µg/ml) with 4-OH, 3-OCH3, and o-hydroxy substituents, respectively, exhibit good activity against S. aureus, while compound 2c containing p-nitro substituent was found to be the most active (MIC 12.5 µg/ml) against B. subtilis. In Gram-negative bacterial strains, compound 3b (o-chloro) was extremely potent (MIC 12.5 µg/ml) against P. pneumonia while compound 2d containing the p-hydroxy group shows excellent activity (MIC 12.5 µg/ml) against E.coli

DOI

10.21608/bfsa.2023.300922

Keywords

Thioglycoolic acid, thiourea, thiosemicarbazide, cyclohexanone, Substituted Aromatic aldehyde

Authors

First Name

Krishna

Last Name

Srivastava

MiddleName

-

Affiliation

Department of Chemistry, Shri Ramswaroop Memorial University, Barabanki, 222502, U.P., India

Email

rintu_srivastava@rediffmail.com

City

-

Orcid

-

First Name

Ram

Last Name

Prakash

MiddleName

-

Affiliation

Department of Chemistry, Shri Ramswaroop Memorial University, Barabanki, 222502, U.P., India

Email

prakashnational48@gmail.com

City

-

Orcid

-

First Name

Raj

Last Name

Singh

MiddleName

Bahadur

Affiliation

Department of Chemistry, Shri Ramswaroop Memorial University, Barabanki, 222502, U.P., India

Email

rajrajpoot133@gmail.com

City

-

Orcid

-

First Name

Abhishek

Last Name

Srivastava

MiddleName

-

Affiliation

Department of Chemistry, GLA University, Mathura 281406, U.P., India

Email

aabhichem@gla.ac.in

City

-

Orcid

-

First Name

Rishi

Last Name

Vishnoi

MiddleName

kumar

Affiliation

Department of Chemistry, Lucknow University, Lucknow, 226007, U.P., India

Email

rk.vchem@gmail.com

City

-

Orcid

-

Volume

46

Article Issue

1

Related Issue

41495

Issue Date

2023-06-01

Receive Date

2022-08-02

Publish Date

2023-06-01

Page Start

203

Page End

216

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 46_Issue 1_Pages 203-216.pdf

PDF . 1.1MB

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https://bpsa.journals.ekb.eg/article_300922.html

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https://bpsa.journals.ekb.eg/service?article_code=300922

Order

300,922

Type

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, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING

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Article

Created At

25 Dec 2024