Synthesis, Docking and Antimicrobial Activity Studies of Some Novel Fused Thiophenes of Biological Interest

    Published on:June 2020
    Journal of Young Pharmacists, 2020; 12(2):118-124
    Original Article | doi:10.5530/jyp.2020.12.24

    Anitha Ramalingam1*, Janardhanan Sarvanan2

    1School of Pharmaceutical Sciences, Dayananda Sagar University, Kumaraswamy Layout, Bangalore, Karnataka, INDIA.

    2Faculty of Pharmaceutical Sciences, PES University, HN Campus, Bangalore, Karnataka, INDIA.


    Objective: Thiophenes are a part of many natural and synthetic biologically active products displaying several pharmacological activities. Area of antibacterial and antifungal research is still on because of faster development of drug resistance of existing molecules by the microbes. Methods: The starting material 2 -amino-3-carbethoxy-6-N- methyl piperidino thiophene[1] was synthesized by adapting a well-known and versatile Gewald’s reaction with excellent yield (85-98%). The title compounds (1 a-l) were obtained by treating the starting material[1] with various arylaldehydes, as per Scheme 1. Structures of the synthesized compounds were confirmed by physical (Lassaigne’s test, MP and Rf vaiues) and spectral data (IR, UV, NMR, Mass and CHN Analyses) and all the new compounds were studied for molecular docking and screened for antimicrobial activity. Results: Among the new compounds, the compounds 1f, 1j and 1l exhibited good activity against pathogenic bacteria and fungi. Discussion The aim of designing and synthesizing new molecules as antimicrobials is because of predominant resistance of bacteria and fungi against the existing drugs using Gewald’s and Schiff’s Reaction. Conclusion: It is concluded that some of the new piperidino thiophene analogues reported here displayed promising activity.

    Key words: Synthesis, Docking, Piperidino thiophene, Gewald’s reaction, Antimicrobial activity.

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