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Bioorg Med Chem Lett. 2011 Apr 1;21(7):1969-73. doi: 10.1016/j.bmcl.2011.02.030. Epub 2011 Feb 13.

Development of selective and reversible pyrazoline based MAO-B inhibitors: virtual screening, synthesis and biological evaluation.

Author information

1
Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835 215, India. nmishra@bitmesra.ac.in

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 K(i) values were observed.

PMID:
21377879
DOI:
10.1016/j.bmcl.2011.02.030
[Indexed for MEDLINE]

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