Recent progress in the discovery of macrocyclic compounds as potential anti-infective therapeutics [PDF]
, 2009 Novel therapeutic strategies are urgently needed for the treatment of serious diseases caused by viral, bacterial and parasitic infections, because currently used drugs are facing the problem of rapidly emerging resistance.
Bernardini, F +6 more
core +1 more source
Synthesis and characterization of novel dipeptide mimetics with hydantoin moiety
Comptes Rendus. Chimie, 2010 The synthesis of three novel 5,5-dimethylhydantoin derivatives 2-amino-N-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)acetamide, 2-amino-N-(4,4-dimethyl-2,5-dioxoimidazol idin-1-yl)-3-phenylpropanamide, and 2-amino-4-methyl-N-(4,4-dimethyl-2,5-dioxoimidazol idin-1-yl) pentanamide, is reported.
Petar T. Todorov, Emilia D. Naydenova
openaire +1 more source
Фармакокинетика и Фармакодинамика, 2020 The present work was to study the GSB-106 effect on the immobility behavior of mice Balb/c in the Porsolt test. GSB-106 was administered sub-chronically and chronically intraperitoneal in dose 1 mg/kg.
A. V. Tallerova +4 more
doaj +1 more source
Peptidomimetic and Organometallic Derivatives of Primaquine Active against Leishmania infantum [PDF]
, 2012 The current treatment of visceral leishmaniasis is made difficult by the low efficacy, elevated costs, low bioavailability, and high toxicity of many of the available drugs.
Ana Tomas +6 more
core +1 more source
An α-Helix-Mimicking 12,13-Helix: Designed α/β/γ-Foldamers as Selective Inhibitors of Protein-Protein Interactions [PDF]
, 2016 A major current challenge in bioorganic chemistry is the identification of effective mimics of protein secondary structures that act as inhibitors of protein–protein interactions (PPIs).
Altmayer-Henzien +47 more
core +2 more sources
Synthetic Strategies for Activity‐Based Probes to Decode Ubiquitin‐Like Modifiers
Chemistry – A European Journal, EarlyView.ABSTRACT Ubiquitin‐like proteins (Ubls) such as SUMO, NEDD8, ISG15, URM1, UFM1, FAT10, ATG8/ATG12, and FUBI are essential regulators of cellular homeostasis, controlling processes from protein stability and trafficking to immune signaling and autophagy.
Saibal Chanda +5 more
wiley +1 more source
Multicomponent dipeptide hydrogels as extracellular matrix-mimetic scaffolds for cell culture applications [PDF]
Chemical Communications, 2015 Fmoc-3F-Phe-Arg-NH2 and Fmoc-3F-Phe-Asp-OH dipeptides undergo coassembly to form two-component nanofibril hydrogels.
Wathsala, Liyanage +4 more
openaire +2 more sources
Chemical Ligation of Backbone N‐hydroxylated Peptides
Chemistry – A European Journal, EarlyView.Peptide backbone N‐hydroxylation enables sequence‐agnostic fragment ligation via hydroxamate O‐acyl capture and O→N acyl transfer in water. Broad tolerance of sterically demanding nucleophilic residues is observed, and reductive N─O cleavage restores the native amide bond.
Natalia Cano‐Sampaio +1 more
wiley +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
British Journal of Pharmacology, EarlyView.Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Stringent Nucleotide Recognition by the Ribosome at the Middle Codon Position. [PDF]
, 2017 Accurate translation of the genetic code depends on mRNA:tRNA codon:anticodon base pairing. Here we exploit an emissive, isosteric adenosine surrogate that allows direct measurement of the kinetics of codon:anticodon University of California base ...
Cooperman, Barry S +5 more
core +3 more sources