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Synthesis and structure-activity relationships of novel neocryptolepine derivatives

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Chemical Research in Chinese Universities Aims and scope

Abstract

Herein we reported the synthesis of a novel series of neocryptolepine(5-methyl-5H-indolo[2,3-b]quinoline) derivatives containing different substituents at C11 using methyl 1H-indole-3-carboxylate and N-methylaniline as starting material. The target 21 compounds were evaluated for their antibacterial activity in vitro against gram-positive bacteria(B. subtilis and S. aureus) and gram-negative bacteria(E.coli and S. typhi). Almost all the tested compounds showed moderate to high activities against the four bacterial strains at the minimum inhibitory concentrations(MICs) of 1—10 μg/mL. The obtained results suggest that part of the novel synthetic neocryptolepine derivatives exhibit significant antibacterial effect against all the tested organisms.

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Acknowledgments

The authors thank Professor Adel El Sayed El Beltagy, Laboratory of Microbiology, El-Menoufia University, and Faculty of Agriculture for performing the antibacterial test.

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Authors and Affiliations

  1. Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Koam, Menoufia, Egypt

    Ahmed A. El-Gokha, Nader M. Boshta, Mona K. Abo Hussein & Ibrahim El-T. El Sayed

  2. Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Eberhard Karls Universität Tübingen, Tübingen, 72076, Germany

    Ahmed A. El-Gokha

  3. Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, Bonn, 53121, Germany

    Nader M. Boshta

Authors
  1. Ahmed A. El-Gokha
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  2. Nader M. Boshta
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  3. Mona K. Abo Hussein
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  4. Ibrahim El-T. El Sayed
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Corresponding author

Correspondence to Ahmed A. El-Gokha.

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40242_2017_6502_MOESM1_ESM.pdf

Using neocryptolepine scaffold as antimicrobial agent: Synthesis and structure-activity relationships of some novel neocryptolepine derivatives

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El-Gokha, A.A., Boshta, N.M., Abo Hussein, M.K. et al. Synthesis and structure-activity relationships of novel neocryptolepine derivatives. Chem. Res. Chin. Univ. 33, 373–377 (2017). https://doi.org/10.1007/s40242-017-6502-6

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  • DOI: https://doi.org/10.1007/s40242-017-6502-6

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