This paper describes the synthesis and structure-activity relationships (SAR) leading to the
first rational design of “dipeptoid" analogues of the neuropeptide cholecystokinin (CCK). …

This paper describes the synthesis and physical and biological effects of introducing different
substituents at the α-position of the tryptophan containing neurokinin-1 receptor antagonist […

The effects of PD 176252 [3-(1H-indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(nitro-phenyl)ureido]propionamide],
a nonpeptide bombesin (BB) BB 1 /BB 2 …

Tauopathies are a group of neurodegenerative disorders characterized by the aggregation of
the microtubule-associated protein tau. Aggregates of misfolded tau protein are believed to …

The use of a dipeptide library as the source of a micromolar chemical lead compound for the
human tachykinin NK 3 receptor is described. The screening of a dipeptide library through a …

We have previously described the design and development of CI-988, a peptoid analogue
of CCK-4 with excellent binding affinity and selectivity for the CCK-B receptor. Due to its …

α-Bromo amides derived from Oppolzer's camphorsultam can be prepared diastereoselectively
starting from racemic α-bromo acids, and undergo epimerisation under appropriate …

The rational design of a non-peptide tachykinin NK 1 receptor antagonist, [(2-benzofuran)-CH
2 OCO]-(R)-α-MeTrp-(S)-NHCH(CH 3 )Ph (28, PD 154075) is described. Compound 28 …

Two classes of structurally different tachykinin neurokinin3 (NK3) antagonists were used to
evaluate species difference in antagonist binding between human and rat NK3 receptors. In …

In this paper a broadly applicable synthesis of chiral α,α-disubstituted amino acids is outlined
based upon regioselective ring opening of aziridine derivatives. Examples of nitrogen, …