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Medicinal Chemistry Research

, Volume 27, Issue 5, pp 1504–1516 | Cite as

Dipeptides as linker for multicomponent presentation—a facile, robust, and high-bioactivity yielding strategy

  • Honnegowdanahally K. Kumara
  • Suhas Ramesh
  • Doddahindaiah M. Suyoga Vardhan
  • J. Shiva Kumar
  • Dase Channe Gowda
Original Research
  • 83 Downloads

Abstract

The need for multiple drugs arises when the response to pharmacological inflection is complicated and the disease conditions get worsened. The treatment requires a common platform to which multiple drugs are linked and this methodology is proven to be useful in drug delivery, biomaterial research, biomedicine, and vaccine development. In view of this, the present work is centered on dipeptides (KW/ KD/ KE/ kW/ kD/ kE), which are used as linkers and can potentially hold different functional group containing molecules (here, amino and carboxyl). First, we have demonstrated the incorporation of three components to the linker successfully followed by tetra component linking to those dipeptides, which contain trifunctional groups. To provide a proof of concept, these multisubstituted constructs were subjected to microbial growth suppression assay as well as anti-inflammatory assay. The biological results revealed that the multimers play a key role in enhancing the activity. Hence, the present system may be regarded as simple and straight forward which can be employed to develop various therapeutic agents as well as in different methodologies.

Keywords

Multicomponent Dipeptides Linker Bioactivity 

Abbreviations

EDCI

1-(3-Dimethylaminopropyl)-3-ethyl-carbodiimide

HOBt

1-Hydroxy benzotriazole

NMM

N-Methylmorpholine

QZN 1

3-(4-Oxo-3,4-dihydroquinazolin-2-yl)propanoic acid

QZN 2

4-(4-Oxo-3,4-dihydroquinazolin-2-yl)butanoic acid

Notes

Acknowledgements

We gratefully acknowledge Department of Science and Technology (DST) New Delhi for awarding Inspire Fellowship, University Grant Commission (UGC) New Delhi for awarding BSR faculty fellowship and UGC-Post doctoral Fellowship (PDFSS). We also acknowledge DST-Purse and Instrumentation facility.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

44_2018_2168_MOESM1_ESM.docx (7.7 mb)
Supplementary Information(DOCX 7906 kb)

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • Honnegowdanahally K. Kumara
    • 1
  • Suhas Ramesh
    • 1
  • Doddahindaiah M. Suyoga Vardhan
    • 1
  • J. Shiva Kumar
    • 1
  • Dase Channe Gowda
    • 1
  1. 1.Department of Studies in ChemistryUniversity of MysoreMysuruIndia

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