J M Bentley

Publications (3)7.66 Total impact

• Article: Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.

  Hans G F Richter, D R Adams, A Benardeau, M J Bickerdike, J M Bentley, T J Blench, I A Cliffe, C Dourish, P Hebeisen, G A Kennett, [......], C S Malcolm, P Mattei, A Misra, J Mizrahi, N J T Monck, J-M Plancher, S Roever, J R A Roffey, S Taylor, S P Vickers
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  ABSTRACT: Further lead optimization efforts on previously described 1,2,3,4,10,10a-hexahydro-1H-pyrazino[1,2-a]indoles led to the new class of 5,5a,6,7,8,9-hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines culminating in the discovery of (5aR,9R)-2-[(cyclopropylmethoxy)methyl]-5,5a,6,7,8,9-hexahydro-9-methyl-pyrido[3', 2':4,5]pyrrolo[1,2-a]pyrazine 18 as a potent, full 5-HT(2C) receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.
  Bioorganic & Medicinal Chemistry Letters 04/2006; 16(5):1207-11. · 2.55 Impact Factor
• Source

  Available from: ihug.co.nz

  Article: Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.

  S Röver, D R Adams, A Bénardeau, J M Bentley, M J Bickerdike, A Bourson, I A Cliffe, P Coassolo, J E P Davidson, C T Dourish, [......], A R Knight, C S Malcolm, P Mattei, A Misra, J Mizrahi, M Muller, R H P Porter, H Richter, S Taylor, S P Vickers
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  ABSTRACT: Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT(2) receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT(2C) receptor agonists.
  Bioorganic & Medicinal Chemistry Letters 09/2005; 15(15):3604-8. · 2.55 Impact Factor
• Source

  Available from: Jon Roffey

  Article: Indoline derivatives as 5-HT(2C) receptor agonists.

  J M Bentley, D R Adams, D Bebbington, K R Benwell, M J Bickerdike, J E P Davidson, C E Dawson, C T Dourish, M A J Duncton, S Gaur, [......], A R Knight, C S Malcolm, H L Mansell, A Misra, N J T Monck, R M Pratt, K Quirk, J R A Roffey, S P Vickers, I A Cliffe
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  ABSTRACT: A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT(2) receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration.
  Bioorganic & Medicinal Chemistry Letters 06/2004; 14(9):2367-70. · 2.55 Impact Factor