SYNTHESIS AND SCREENING OF BENZOFURAN FUSED C-2,4,6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS A NEW ANTIBACTERIAL AND ANTIFUNGAL AGENT


Javarappa Rangaswamy, Nagaraja Naik

Abstract


Objective: Benzofuran and their heterocyclic analogs represent an important class of molecules which have a wide range of pharmacological activities. Therefore, in this study synthesis and antimicrobial activity of benzofuran fused C-2,4,6-substituted pyrimidine derivatives was extensively discussed.

Methods: Benzofuran fused C-2,4,6-substituted pyrimidine derivatives (4a-k) were built by cyclo condensation, Claisen-Schmidt condensation followed by cyclization via coupling of benzoyl fragments, which include benzofuran, a pyrimidine ring and C-6 substituted phenyl residue with various substituents, connected by linker-S-band. The structures of the synthesized compounds were confirmed by analytical and spectral techniques and evaluated their antimicrobial activity.

Results: The results of antibacterial and antifungal activity against various microbes, most of the compounds have shown considerable antimicrobial activity, but compounds 4g and 4e exhibits superior activity compared to standards, this may be due to presence bromo and fluro electron withdrawing substituent on the benzoyl moiety and more lipophilic nature of pyrimidine ring.

Conclusion: According to the activity studies, it is observed that the synthesis and antimicrobial activity of benzofuran fused C-2,4,6-substituted pyrimidine derivatives have been shown better antimicrobial activity. The obtained results suggest that these classes of compounds can be considered as new hits for further structural optimization to obtain better antimicrobial drug development program.


Keywords


Benzofuran incorporating substituted pyrimidines, Substituted benzoyl moieties, Antimicrobial activity

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About this article

Title

SYNTHESIS AND SCREENING OF BENZOFURAN FUSED C-2,4,6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS A NEW ANTIBACTERIAL AND ANTIFUNGAL AGENT

Keywords

Benzofuran incorporating substituted pyrimidines, Substituted benzoyl moieties, Antimicrobial activity

DOI

10.22159/ijpps.2017v9i9.17487

Date

13-07-2017

Additional Links

Manuscript Submission

Journal

International Journal of Pharmacy and Pharmaceutical Sciences
Vol 9, Issue 9, 2017 Page: 27-32

Online ISSN

0975-1491

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70 Views | 31 Downloads

Authors & Affiliations

Javarappa Rangaswamy
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore – 570006, Karnataka, India
India

Nagaraja Naik
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore – 570006, Karnataka, India
India


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