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Research on Chemical Intermediates

, Volume 44, Issue 5, pp 3349–3364 | Cite as

Synthesis, antileishmanial and cytotoxicity activities of fused and nonfused tetrahydroquinoline derivatives

  • Hassan Mohamed Fawzy Madkour
  • Maher Abd El-Aziz Mahmoud El-Hashash
  • Marwa Sayed Salem
  • Al-Shimaa Omar Ali Mahmoud
Article
  • 113 Downloads

Abstract

Developing novel antileishmanial, and cytotoxic drugs has been a significant area in modern pharmaceutical research. A series of novel triazolo[4,3-a]quinoline, triazino[4,3-a]quinoline, thiadiazepino[5,6-b]quinoline and pyrazolquinoline have been synthesized from the reaction of 2-hydrazinyltetrahydroquinoline-3-carbonitrile with formamide, formic acid, ethyl chloroacetate, carbon disulphide in an alcoholic solution of potassium hydroxide acetyl acetone and/or ethyl cyanoacetate, respectively. These compounds were evaluated for their in vitro studies against L. major leishmanial. The brine shrimp bioassay was also conducted to study their in vitro cytotoxic properties which displayed potent cytotoxic activity against Vincristine. The newly synthesized compounds were all characterized through IR, 1H-NMR, and MS.

Keywords

Tetrahydroquinolines Triazolo[4,3-a]quinoline Triazino[4,3-a]quinoline Thiadiazepino[5,6-b]quinoline Antileishmanial Cytotoxicity 

Notes

Acknowledgements

The authors gratefully thank Dr. Muhammad Ashfaq and Dr. Yasser MSA Alkahraman, Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad, Pakistan for performing antileishmanial and cytotoxicity screening of the synthesized compounds.

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Copyright information

© Springer Science+Business Media B.V., part of Springer Nature 2018

Authors and Affiliations

  • Hassan Mohamed Fawzy Madkour
    • 1
  • Maher Abd El-Aziz Mahmoud El-Hashash
    • 1
  • Marwa Sayed Salem
    • 1
  • Al-Shimaa Omar Ali Mahmoud
    • 1
  1. 1.Synthetic Organic Chemistry Laboratory, Chemistry Department, Faculty of ScienceAin Shams UniversityAbbassia, CairoEgypt

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