Nuzzi, Andrea; Fiasella, Annalisa; Ortega, Jose Antonio; Pagliuca, Chiara; Ponzano, Stefano; Pizzirani, Daniela; Bertozzi, Sine Mandrup; Ottonello, Giuliana; Tarozzo, Glauco; Reggiani, Angelo; Bandiera, Tiziano; Bertozzi, Fabio; Piomelli, Daniele published the artcile< Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies>, Quality Control of 52244-70-9, the main research area is amino lactam carbamic acid ester acylethanolamine acid amidase inhibitor; Carbamates; Cysteine hydrolase; Inhibitors; N-acylethanolamine acid amidase; Structure–activity relationships; β-lactams.
4-Cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate I is a potent, selective and systemically active inhibitor of intracellular NAAA activity, which produces profound anti-inflammatory effects in animal models. In the present work, the authors describe structure-activity relationship (SAR) studies on 3-aminoazetidin-2-one derivatives, which have led to the identification of I, and expand these studies to elucidate the principal structural and stereochem. features needed to achieve effective NAAA inhibition. Investigations on the influence of the substitution at the β-position of the 2-oxo-3-azetidinyl ring as well as on the effect of size and shape of the carbamic acid ester side chain led to the discovery of II, a novel inhibitor of human NAAA that shows an improved physicochem. and drug-like profile relative to I. This favorable profile, along with the structural diversity of the carbamic acid chain of I, identify this compound as a promising new tool to investigate the potential of NAAA inhibitors as therapeutic agents for the treatment of pain and inflammation.
European Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Quality Control of 52244-70-9.
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