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The use of γ-turn mimetics to define peptide secondary structure
Abstract A novel γ-turn mimetic 2 has been prepared based on retro amide peptide design. Incorporation of this mimetic into linear peptide fibrinogen receptor antagonist 7 (GPIIb/IIIa receptor)
Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore.
Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.
TLDR
The overall data suggest that the features contributing to the observed high potency in this series are the orientation of the 3-4 amide and the conformational constraint imposed by the seven-membered ring, both of which position the key acidic and basic groups in the proper spatial relationship.
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists.
TLDR
A series of prolyl-1-piperazinylacetic acid and prolylate derivatives were synthesized and evaluated for their activity as VLA-4 antagonists, and 19 compounds showed potent activity with low nanomolar IC50 values.
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.
An investigation into the structure-activity relationship of a lead compound, prolyl-5-aminopentanoic acid 4, led to the identification of a novel series of 4-piperidinylacetic acid,
Design, synthesis and SAR of RGD peptide hybrids as highly efficient inhibitors of platelet aggregation
Abstract A new series of peptide hybrids is developed as highly potent and selective antagonists of the GPIIb/IIIa receptor through rational modification of the RGDX sequence. Structure-activity
Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series
Abstract In an investigation of the contribution of N-1 to the binding, antiaggregatory, and oral activity in 3-oxo-1,4-benzodiazepine-2-acetic acid based GPIIb/IIIa antagonists, a series of
Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5).
TLDR
High-throughput screening of an extensive series of ECLiPStrade mark compound libraries led to the identification of compound 1 as a dual inhibitor of the alpha(v)-integrinsalpha(v) beta(3) and alpha( v)beta(5) and the discovery of compounds 15a and 15b with reduced PSA and much improved potency.
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