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TATB and TBMT are very suitable for the preparation of more soluble bicyclic peptides.
2
Our approach should be generally applicable to developing cell-permeable bicyclic peptide inhibitors against other intracellular proteins.
3
Several carboxamides derived from this bicyclic scaffold displayed improved antiviral activity and pharmacokinetic profiles when compared with corresponding spirocyclic analogs.
4
Using a pharmacophore model containing a bicyclic amine as anchor, we designed a series of amide antagonists with targeted physicochemical properties.
5
We report here a methodology for chemical synthesis and screening of large combinatorial libraries of bicyclic peptides displayed on rigid small-molecule scaffolds.
6
Medium-sized ynolides were prepared by the Lewis acid-mediated fragmentation of bicyclic γ-silyloxy-β-hydroxy-a-diazolactones in which the Cβ-Cγ bond is the ring fusion bond.
7
Two polar hinges for cyclization of peptides have been developed, leading to bicyclic peptides and cyclized peptides with improved solubility and biological activity.
8
Fusion of cyclic peptides with a cyclic cell-penetrating peptide produces bicyclic peptides that are cell-permeable and retain the ability to recognize specific intracellular targets.
9
With planar trimesic acid as the scaffold, the resulting bicyclic peptides are effective for binding to protein surfaces such as the interfaces of protein-protein interactions.
10
When the activities of the bicyclic debranones were compared in the same two assays, one was more active than GR24 in the rice tillering assay.
11
The N-substituted 4-aminocoumarin bicyclic and tricyclic derivatives 5-8 were prepared by treating the corresponding chloro derivatives with the excess suitable amines.
12
We have previously reported on sulfonamide and sulfone-based B1 antagonists containing a privileged bicyclic amine moiety leading to potent series of 2-oxopiperazines.
13
The structure of 1 was determined by NMR spectroscopic analyses as a prodigiosin derivative with the same bicyclic alkyl chain as 2.
14
These more highly constrained bicyclic systems give new insight into the details of molecular recognition of residues 3-5 of angiotensin by the receptor.
15
Bicyclic peptides of this type may provide a general solution for inhibition of protein-protein interactions.
16
TATB and TBMT are very suitable for the preparation of more soluble bicyclic peptides.