Tiziana Scoccitti

Publications (2)5.3 Total impact

• Article: The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.

  John Skidmore, Zeenat Atcha, Emmanuelle Boucherat, Laura Castelletti, Deborah W Chen, Frank T Coppo, Leanne Cutler, Rachel M Dunsdon, Bronagh M Heath, Rio Hutchings, [......], David Norton, Darrel J Pemberton, Sally Redshaw, Richard Rutter, Sanjeet S Sehmi, Tiziana Scoccitti, Hannah E Temple, Pam Theobald, Robert W Ward, David M Wilson
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  ABSTRACT: A series of α7 nicotinic acetylcholine receptor full agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Early lead 1 was found to have a limited therapeutic index with respect to its potential for cardiovascular side effects. Further optimisation of this series led to the identification of 22 a potent full agonist showing efficacy at a dose of 0.1mg/kg in the novel object recognition model of cognition enhancement. Comparison of 1 with 22 demonstrated the latter to have an improved oral pharmacokinetic profile and cardiovascular therapeutic index.
  Bioorganic & medicinal chemistry letters 03/2012; 22(10):3531-4. · 2.65 Impact Factor
• Article: Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.

  John Skidmore, Zeenat Atcha, Emmanuelle Boucherat, Laura Castelletti, Deborah W Chen, Frank T Coppo, Leanne Cutler, Rachel M Dunsdon, Bronagh M Heath, Rio Hutchings, [......], David Norton, Darrel J Pemberton, Sally Redshaw, Richard Rutter, Sanjeet S Sehmi, Tiziana Scoccitti, Hannah E Temple, Pam Theobald, Robert W Ward, David M Wilson
  [show abstract] [hide abstract]
  ABSTRACT: A series of α7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both α7 potency and selectivity with respect to interaction with the hERG channel are described. Further profiling led to the identification of compound 22, a potent full agonist showing efficacy in the novel object recognition model of cognition enhancement.
  Bioorganic & medicinal chemistry letters 03/2012; 22(10):3560-3. · 2.65 Impact Factor