A review on design, synthesis and pharmacological effect of novel Coumarins derivatives

Farook Mohd 1*, Ashish Pathak 1, Nida Khan2

Department of Pharmaceutical Chemistry ,Ravishankar college of Pharmacy, Bhopal, Madhyapradesh, India

Refer this article

Farook Mohd, Ashish Pathak, Nida Khan, 2013. A review on design, synthesis and pharmacological evaluation of novel coumarins derivatives. Journal of medical pharmaceutical and allied sciences, V 2 - I 3, Pages -67 – 72. Doi: https://doi.org/10.55522/jmpas.v2i3.0019.

ABSTRACT

With the aim to find out the structural features for the MAO inhibitory activity and selectivity, in the present communication we report the design, synthesis and pharmacological evaluation review of a new series of 2-H-Chromen-2-one 4- methyl-2H-chromen-2-one Coumarin derivatives without substituent and with different number of methoxy substituent in the 3-phenyl ring, 3,4-dihydrocoumarin. The substituent in this new scaffold was introduced in the 3’, 4’ and/or 5’ positions of the 3-phenyl ring of the coumarin moiety. The synthesized compounds 3-6 were evaluated as MAO A and B inhibitors using R-(-)-deprenyl (selegiline) and Iproniazide as reference inhibitors, showing, most of them, MAO-B inhibitory activities in the nanomolar range. Compounds 3 (11.05±0.81 nM), 4 (3.23±0.49 nM) and 5 (7.12±0.01 nM) show higher activity than selegiline (IC50 = 19.60 nM), and high MAO-B selectivity with 9,050- fold, 30,960-fold and 14,045-fold inhibition levels, with respect to the MAO-A isoform.

Keywords:

Coumarin, MAO-B Inhibitor, QSAR approach, therapeutically active

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