Development of selective and reversible pyrazoline based MAO-B inhibitors: virtual screening, synthesis and biological evaluation |
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Authors: | Mishra Nibha Sasmal D |
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Affiliation: | Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835 215, India |
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Abstract: | In an effort to develop selective MAO (monoamine oxidase) B inhibitors, structure based virtual screening was initiated on an in-house library. Top 10 HITS were synthesized and evaluated for MAO (A and B) inhibitory activity, both against human and rat enzymes. All the compounds were found selective, reversible and active in nM range (100 times more potent than selegeline) towards MAO-B. Outstanding co-relation between predicted and experimental Ki values were observed. |
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Keywords: | Pyrazoline Monoamine oxidase Virtual screening |
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