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

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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.

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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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Authors and Affiliations

  1. Synthetic Organic Chemistry Laboratory, Chemistry Department, Faculty of Science, Ain Shams University, Abbassia, Cairo, 11566, Egypt

    Hassan Mohamed Fawzy Madkour, Maher Abd El-Aziz Mahmoud El-Hashash, Marwa Sayed Salem & Al-Shimaa Omar Ali Mahmoud

Authors
  1. Hassan Mohamed Fawzy Madkour
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  2. Maher Abd El-Aziz Mahmoud El-Hashash
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  3. Marwa Sayed Salem
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  4. Al-Shimaa Omar Ali Mahmoud
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Correspondence to Marwa Sayed Salem.

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Madkour, H.M.F., El-Hashash, M.A.EA.M., Salem, M.S. et al. Synthesis, antileishmanial and cytotoxicity activities of fused and nonfused tetrahydroquinoline derivatives. Res Chem Intermed 44, 3349–3364 (2018). https://doi.org/10.1007/s11164-018-3311-6

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  • DOI: https://doi.org/10.1007/s11164-018-3311-6

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