Synthesis, leishmanicidal and enzyme inhibitory activities of quinoline-4-carboxylic acids. | [Journal of Chemical Society of Pakistan • 2009]

Author(s):

1. Khalid Mohammad Khan: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences (ICCBS), University of Karachi, Karachi, Pakistan

2. Uzma Rasool Mughal: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences (ICCBS), University of Karachi, Karachi, Pakistan

3. Samreen: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences (ICCBS), University of Karachi, Karachi, Pakistan

4. Ajmal Khan: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences (ICCBS), University of Karachi, Karachi, Pakistan

5. Sumayya Saied: Department of Chemistry, University of Karachi, Karachi, Pakistan

6. Marium Munawar: Department of Chemistry, University of Karachi, Karachi, Pakistan

7. Shahnaz Perveen: Pakistan Council of Scientific & Industrial Research, PCSIR Laboratories Complex, Karachi, Pakistan

Abstract:

A series of quinoline-4-carboxylic acids 1-13 was synthesized and screened for their leishmanicidal, phosphodiesterase, fl-glucuronidase and urease inhibitory properties. Only compounds 3 and 7 were found to be active against leishmaniasis with IC50 values of 76.26 ± 0.71 and 62.86 ± 0.35, µg/mL, respectively. In phosphodiesterase assay only compound 13 showed maximum percentage inhibition (47.2%) among all the tested compounds. Compound 9 showed maximum percentage inhibition value (47.4%) against fl-glucuronidase enzyme. Compound 13 showed maximum percentage inhibition value i.e. 14.10 % against urease enzyme. The structures of all the synthetic compounds were deduced by spectroscopic techniques, including `H NMR, El-MS, IR, and UV spectroscopy.

Page(s): 809-818

DOI: DOI not available

Published: Journal: Journal of Chemical Society of Pakistan, Volume: 31, Issue: 5, Year: 2009

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