Results 21 to 30 of about 6,642 (186)

Improvement on Permeability of Cyclic Peptide/Peptidomimetic: Backbone N-Methylation as A Useful Tool

open access: yesMarine Drugs, 2021
Peptides have a three-dimensional configuration that can adopt particular conformations for binding to proteins, which are well suited to interact with larger contact surface areas on target proteins.
Yang Li, Wang Li, Zhengshuang Xu
doaj   +1 more source

A readily applicable strategy to convert peptides to peptoid-based therapeutics. [PDF]

open access: yesPLoS ONE, 2013
Incorporation of unnatural amino acids and peptidomimetic residues into therapeutic peptides is highly efficacious and commonly employed, but generally requires laborious trial-and-error approaches.
Minyoung Park   +3 more
doaj   +1 more source

Backbone Steric Constraints Underlie High Passive Membrane Permeability of N‐Alkyl Peptides

open access: yesAngewandte Chemie, EarlyView.
Beyond amide hydrogen removal, steric constraints encoded in N/Cα‐dually substituted backbones are uncovered as a key determinant of passive membrane permeability in N‐alkyl peptides. These constraints restrict conformational freedom and sterically limit backbone hydration during membrane permeation.
Ayumi Inayoshi   +8 more
wiley   +2 more sources

Borylcyclopropanes: Synthetic Strategies and Applications

open access: yesAngewandte Chemie, EarlyView.
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley   +2 more sources

Azole γ‐Peptides Helix Switching via Heterocycle Substitutions

open access: yesAngewandte Chemie, EarlyView.
Heterocycle substitution in azole‐based γ‐amino acids enables control over the helical shape of heterocyclic γ‐peptides. S↔N permutation in thiazole residues switches a canonical 9‐helix into a flexible helix exhibiting discontinuous hydrogen bonding.
Samantha Chaise   +10 more
wiley   +2 more sources

Short Cationic Peptidomimetic Antimicrobials

open access: yesAntibiotics, 2019
The rapid growth of antimicrobial resistance against several frontline antibiotics has encouraged scientists worldwide to develop new alternatives with unique mechanisms of action. Antimicrobial peptides (AMPs) have attracted considerable interest due to
Rajesh Kuppusamy   +3 more
doaj   +1 more source

Peptides and peptidomimetics as prototypes [PDF]

open access: yesCurrent Opinion in Chemical Biology, 2008
Since the unraveling of the structure of the α-helix [1] and β-sheet [2] by smart modeling, the use of peptides and their mimetics has been a highly fruitful approach that continues to attract natural scientists. These molecules occupy a privileged place in chemical biology, being both readily accessible via chemical synthesis and directly relevant to ...
Helma, Wennemers, Ronald T, Raines
openaire   +2 more sources

Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics

open access: yesBeilstein Journal of Organic Chemistry, 2014
In the recent past, the design and synthesis of peptide mimics (peptidomimetics) has received much attention. This because they have shown in many cases enhanced pharmacological properties over their natural peptide analogues.
Gijs Koopmanschap   +2 more
doaj   +1 more source

The Use of Peptides in the Treatment of Fragile X Syndrome: Challenges and Opportunities

open access: yesFrontiers in Psychiatry, 2021
Fragile X Syndrome (FXS) is the most frequent cause of inherited intellectual disabilities and autism spectrum disorders, characterized by cognitive deficits and autistic behaviors.
Alice Romagnoli, Daniele Di Marino
doaj   +1 more source

Regioselective Cyclic Iminium Formation of Ugi Advanced Intermediates: Rapid Access to 3,4-Dihydropyrazin-2(1H)-ones and Other Diverse Nitrogen-Containing Heterocycles

open access: yesMolecules, 2023
Herein, advanced intermediates were synthesized through Ugi four-component reactions of isocyanides, aldehydes, masked amino aldehyde, and carboxylic acids, including N-protected amino acids.
Naděžda Cankařová, Viktor Krchňák
doaj   +1 more source

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