2. Academic Validation
  3. Synthesis, stereochemical separation, and biological evaluation of selective inhibitors of human MAO-B: 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines

Synthesis, stereochemical separation, and biological evaluation of selective inhibitors of human MAO-B: 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines

  • J Med Chem. 2010 Sep 9;53(17):6516-20. doi: 10.1021/jm100120s.
Franco Chimenti 1,  Daniela Secci,  Adriana Bolasco,  Paola Chimenti,  Arianna Granese,  Simone Carradori,  Matilde Yáñez,  Francisco Orallo,  M Luisa Sanna,  Bruno Gallinella,  Roberto Cirilli
Affiliations

Affiliation

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Universita degli Studi di Roma La Sapienza, P.A. Moro 5, 00185 Roma, Italy.
PMID: 20715818 DOI: 10.1021/jm100120s
Abstract

Novel 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazine derivatives have been investigated for their ability to inhibit selectively the activity of the human B isoform of Monoamine Oxidase. These compounds were obtained as racemates and (R)-enantiomers by a stereoconservative synthetic pattern in high yield and enantiomeric excess. The (S)-enantiomers of the most active derivatives have been separated by enantioselective HPLC. All compounds showed selective activity against hMAO-B with IC(50) ranging between 21.90 and 0.018 microM.

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