Research Articles

Monoamine oxidase-A inhibitory activity of novel Curcumin analogues

Vol. 2 No. 3-4 (2015) 12-17 Published December 11, 2015

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Abstract

Curcumin has been known for its antidepressant activity, but its use has been restricted due to its poor pharmacokinetic properties. In an effort to enhance its permeability and metabolic stability, a series of four novel curcumin analogues (5a-5d) were synthesized. They were tested for their hMAO inhibitory activity as well as for their permeability and metabolic stability characteristics in in vitro models. The newly synthesized compounds were found to be potent when compared with curcumin and also they are selective and reversible towards hMAO-A. Compounds 5c and 5d were found to be potent inhibitors of hMAO-A with Ki values of Ki=0.110.01M and Ki=0.060.002 M and with selectivity index of SIMAO-A=802.36 and SIMAO-A=507.33, respectively. A slight enhancement in metabolic stability is achieved through the chemical modification.

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Author information

  • Vishnu Nayak Badavath

    Ph.D

  • ?pek Baysal

    Haceteppe University

  • Gulberk Ucar

    Haceteppe University

  • Barij Nayan Sinha

    Birla Institute of Technology

  • Susanta Kumar Mondal

    Chembiotech, TCG Life Sciences

  • Venkatesan Jayaprakash

    Birla Institute of Technology

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Badavath, V. N.; Baysal, ?pek; Ucar, G.; Sinha, B. N.; Mondal, S. K.; Jayaprakash, V. Monoamine Oxidase-A Inhibitory Activity of Novel Curcumin Analogues. J Pharm Chem 2015, 2 (3-4), 12-17. https://doi.org/10.14805/jphchem.2015.art46.
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Received
August 7, 2015
Published
December 11, 2015
Section
Research Articles
Pages
12-17

Keywords

  • Curcumin analogue
  • hMAO inhibitors
  • Caco-2 permeability
  • Human liver microsomal metabolic stability

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