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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.

Previously reported studies from these laboratories described the design of a novel series of high-affinity NK1 antagonists based on the 4,4-disubstituted piperidine ring system. Further structure-activity studies have now established that for high NK1 affinity the benzyl ether side chain must be 3,5-disubstituted and highly lipophilic, the optimal side chain being the 3, 5-bis(trifluoromethyl)benzyl ether, 12 (hNK1 IC50 = 0.95 nM). Additional studies have shown that this class of NK1 antagonist tolerates a wider range of substituents on the piperidine nitrogen, including acyl (38) (hNK1 IC50 = 5.3 nM) and sulfonyl (39) (hNK1 IC50 = 5.7 nM) derivatives. Following preliminary pharmacokinetic analysis, two compounds (32 and 43) were selected for in vivo study in the resiniferotoxin-induced vascular leakage model, both showing excellent profiles (ID50 = 0.22 and 0.28 mg/kg, respectively).[1]

References

  1. 4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity. Stevenson, G.I., Huscroft, I., MacLeod, A.M., Swain, C.J., Cascieri, M.A., Chicchi, G.G., Graham, M.I., Harrison, T., Kelleher, F.J., Kurtz, M., Ladduwahetty, T., Merchant, K.J., Metzger, J.M., MacIntyre, D.E., Sadowski, S., Sohal, B., Owens, A.P. J. Med. Chem. (1998) [Pubmed]
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