2. Academic Validation
  3. Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles

Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles

  • Bioorg Med Chem Lett. 2013 Sep 15;23(18):5128-30. doi: 10.1016/j.bmcl.2013.07.035.
Rossella Fioravanti 1,  Nicoletta Desideri,  Mariangela Biava,  Luca Proietti Monaco,  Laura Grammatica,  Matilde Yáñez
Affiliations

Affiliation

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Università La Sapienza, Rome, Italy. rossella.fioravanti@uniroma1.it
PMID: 23927971 DOI: 10.1016/j.bmcl.2013.07.035
Abstract

A series of 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles (3a-k and 4a-u) were designed, synthesized, and evaluated for their inhibitory efficacy towards the two hMAO isoforms. Most of the derivatives were found to be potent and selective hMAO-B inhibitors. In particular, derivative 3g showed greater hMAO-B affinity than selective inhibitor selegiline coupled with high selectivity index (SI=145). The most selective hMAO-B inhibitor was the 3-methyl analogue 3f with an SI higher than 909.

Keywords

Monoamine oxidases; Pyrazole derivatives; hMAO inhibitors.

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