DESIGN, SYNTHESIS, AND PHARMACOLOGICAL EVALUATION OF SOME NOVEL BIS-THIAZOLE DERIVATIVES


Ramesh M Borde, Satish B Jadhav, Rahul R Dhavse, Achut S Munde

Abstract


 Objective: A series of substituted 5,2-bis-thiazoles derivatives were synthesized by Hantzsch reaction and evaluated in vitro for antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus.

Methods: 2-(4-(benzyloxy)phenyl)-4-methylthiazole-5-carbothioamide were synthesized and allowed to react with various α-haloketones to give 5,2-bis-thiazoles, i.e., 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole derivatives in excellent yield. The synthesized compounds were characterized by spectroscopic methods as well as elemental analyses. They were screened for their antimicrobial activity using the agar diffusion method.

Result: Literature survey reveals that the synthesis of 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole, i.e., (5,2-Bis-thiazoles) derivatives (10a-e) was not reported. The entire compound exhibited mild to moderate antimicrobial activity.

Conclusion: The antimicrobial results revealed that the synthesized derivatives have significant antimicrobial properties, and further, structure– activity relationship studies may develop more potent and less toxic molecule.


Keywords


Bis-thiazoles, Thiazolyl-carbothioamide, α-Haloketones, Antimicrobial activity.

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About this article

Title

DESIGN, SYNTHESIS, AND PHARMACOLOGICAL EVALUATION OF SOME NOVEL BIS-THIAZOLE DERIVATIVES

Topics

none

Keywords

Bis-thiazoles, Thiazolyl-carbothioamide, α-Haloketones, Antimicrobial activity.

DOI

10.22159/ajpcr.2018.v11i4.23413

Date

01-04-2018

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 11 Issue 4 April 2018 Page: 164-168

Print ISSN

0974-2441

Online ISSN

2455-3891

Authors & Affiliations

Ramesh M Borde
Department of Chemistry , Milind College of Science, Aurangabad, Maharashtra, India.
India

Satish B Jadhav
Department of Chemistry , Balbhim Arts, Science and Commerce College, Beed, Maharashtra, India
India

Rahul R Dhavse
Department of Chemistry , Milind College of Science, Aurangabad, Maharashtra, India.
India

Achut S Munde
Department of Chemistry , Milind College of Science, Aurangabad, Maharashtra, India.
India


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