Identification of the stereochemical requirements in the 4-aryl-2-cycloalkylidenhydrazinylthiazole scaffold for the design of selective human monoamine oxidase B inhibitors.

@article{DAscenzio2014IdentificationOT,
  title={Identification of the stereochemical requirements in the 4-aryl-2-cycloalkylidenhydrazinylthiazole scaffold for the design of selective human monoamine oxidase B inhibitors.},
  author={Melissa D'Ascenzio and Simone Carradori and Daniela Secci and Luisa Mannina and Anatoly Petrovich Sobolev and Celeste De Monte and Roberto Cirilli and Matilde Y{\'a}{\~n}ez and Stefano Alcaro and Francesco Ortuso},
  journal={Bioorganic & medicinal chemistry},
  year={2014},
  volume={22 10},
  pages={2887-95}
}
Exploring the effect that substituents on the cycloaliphatic ring had on the inhibitory activity against human monoamine oxidase B of a series of 4-aryl-2-cycloalkylidenhydrazinylthiazoles led to the synthesis of a new series of 2-methylcyclopentyl and 3-methylcyclopentyl derivatives which were tested in vitro as mixtures of diastereoisomers. In fact, due to the presence of a chiral center on the cycloaliphatic ring and a trisubstituted CN bond, they exist as four diastereoisomers ((E)-(R), (E… CONTINUE READING