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

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Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.

The 3,5-bis(trifluoromethyl)benzyl ester of N-acetyl-L-tryptophan 1 (L-732,138) has been identified previously as a potent and selective substance P receptor antagonist. A series of analogs which introduced a 6-membered heterocyclic ring into the backbone of this structure were prepared for evaluation as bioisosteric replacements of the ester linkage of 1. The 2,5-dioxopiperazine 2 had very weak receptor affinity, but 2-oxopiperazine 5 exhibited modest activity. Examination of the conformations accessible to the substituents on these templates led to exploration of the corresponding 5-membered heterocyclic rings. This study culminated in the identification of oxazolidinedione 14 as a suitable ester mimic in terms of the retention of good NK1 binding affinity.[1]

References

  1. Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage. Lewis, R.T., Macleod, A.M., Merchant, K.J., Kelleher, F., Sanderson, I., Herbert, R.H., Cascieri, M.A., Sadowski, S., Ball, R.G., Hoogsteen, K. J. Med. Chem. (1995) [Pubmed]
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