Monoamine Oxidase Inhibition and Molecular Modeling Studies of Piperidyl-thienyl and 2-Pyrazoline Derivatives of Chalcones

Author(s): Sumera Zaib , Syed Umar Farooq Rizvi , Sana Aslam , Matloob Ahmad , Mariya al-Rashida , Jamshed Iqbal .

Journal Name: Medicinal Chemistry

Volume 11 , Issue 5 , 2015

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Abstract:

A series of piperidyl-thienyl & 2-pyrazoline derivatives of quinolyl-thienyl chalcones were tested to observe the structural characteristics for the monoamine oxidase inhibitory (MAO) activity. In both these series, a diverse range of substituted thiophenes are used which enable the structure activity relationship. The compounds showed enhanced inhibition against MAO-A & B as compared to reference compounds. Compound 1c exhibited most potent MAO-A inhibition having IC50 value of 0.062 M, while 1j showed excellent inhibitory potency against MAO-B having IC50 value of 0.088 M. The present investigation demonstrated that among piperidyl-thienyl chalcones, almost all the compounds exhibit significant MAO-A inhibition, thus may have antidepressant activity. Whereas among the 2-pyrazoline derivatives of chal-cones, many compounds revealed MAOB inhibition and hence may be applied in the control of senile dementia. Molecular docking studies were carried out against human MAO-A and MAO-B to rationalize important binding site interactions.

Keywords: Antidepressant activity, molecular docking, monoamine oxidase, piperidyl-thienyl derivatives, quinolyl-thienyl chalcones.

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Article Details

VOLUME: 11
ISSUE: 5
Year: 2015
Page: [497 - 505]
Pages: 9
DOI: 10.2174/1573406410666141229101130
Price: $58

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