Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
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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, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series, e.g. I, displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was obsd., within this novel series and a no. of other piperidine bioisosteric cores. <br/> <br/> |
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| Idioma(s) |
eng |
| Direitos |
info:eu-repo/semantics/restrictedAccess |
| Fonte |
Sheffler , D J , Nedelovych , M T , Williams , R , Turner , S C , Duerk , B B , Robbins , M R , Jadhav , S B , Niswender , C M , Jones , C K , Conn , P J , Daniels , R N & Lindsley , C W 2014 , ' Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres ' Bioorganic and Medicinal Chemistry Letters , vol 24 , no. 4 , pp. 1062-1066 . DOI: 10.1016/j.bmcl.2014.01.011 |
| Tipo |
article |
