2-Amino Analogues of Alkynyl Substituted 1,4-dihydropyrimidine: Their Synthesis and Evaluation as Potential Antimicrobial/Cytotoxic Agents

Author(s): V. Mallikarjuna Rao, A. Srinivasa Rao*, P. Ravi Kumar, S. Shobha Rani, Manojit Pal*

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 10 , 2018

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Graphical Abstract:


Background: The past decade has witnessed a significant increase in the prevalence of resistance to antibacterial and antifungal agents. To overcome this problem it is desirable to devote continuing effort in evaluating new series of chemical entities for the identification of new antimicrobial agents.

Methods: The alkynyl substituted 2-amino-1,4-dihydropyrimidine framework has been explored for the identification of potential antimicrobial / cytotoxic agents. Compounds derived from this framework were synthesized using a multi-step method involving the Biginelli reaction, followed by chlorination and subsequent displacement of the chloro group by various amines and finally alkynylation via a Cu-free Sonogashira coupling.

Results: Several of these compounds showed promising antimicrobial / antifungal activities and cytotoxicity against cancer cell lines indicating their potential in reducing the danger of bacterial infections in the immunocompromised cancer patients.

Conclusion: We have shown that the current framework could be an attractive template for the design and generation of diversity based library of small molecules leading.

Keywords: 2-amino-1, 4-dihydropyrimidine, antimicrobial, antifungal, cytotoxicity, sonogashira coupling, alkynylation.

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Article Details

Year: 2018
Published on: 27 August, 2018
Page: [1095 - 1102]
Pages: 8
DOI: 10.2174/1570180814666171121151921
Price: $65

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