Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead
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15/02/2014
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| Resumo |
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach that provided a robust intellectual property position, in lieu of a traditional, expensive HTS campaign. Members within this new [3.1.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, CNS penetration and efficacy in a preclin. model of schizophrenia (prepulse inhibition). <br/> |
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| Idioma(s) |
eng |
| Direitos |
info:eu-repo/semantics/restrictedAccess |
| Fonte |
Jones , C K , Sheffler , D J , Williams , R , Jadhav , S B , Felts , A S , Morrison , R D , Niswender , C M , Daniels , J S & Conn , P J 2014 , ' Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead ' Bioorganic and Medicinal Chemistry Letters , vol 24 , no. 5 , pp. 1067-1070 . DOI: 10.1016/j.bmcl.2014.01.013 |
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article |
