Results 41 to 50 of about 6,642 (186)

1H-Imidazole-2,5-Dicarboxamides as NS4A Peptidomimetics: Identification of a New Approach to Inhibit HCV-NS3 Protease

Biomolecules, 2020
The nonstructural (NS) protein NS3/4A protease is a critical factor for hepatitis C virus (HCV) maturation that requires activation by NS4A. Synthetic peptide mutants of NS4A were found to inhibit NS3 function.
Abdelsattar M. Omar, Mahmoud A. Elfaky, Stefan T. Arold, Sameh H. Soror, Maan T. Khayat, Hani Z. Asfour, Faida H. Bamane, Moustafa E. El-Araby   +7 more
doaj   +1 more source

Temperature-Controlled Diastereoselective Doebner/Ugi Tandem Reaction

SynOpen, 2023
Novel peptidomimetics containing a pyrrolone fragment were synthesized by a tandem combination of Doebner and Ugi type multicomponent reactions with controlled diastereoselectivity. This approach represents a convenient synthesis in the temperature range
Yana Sakhno, Oleksandr Radchenko, Vyacheslav Saraev, Yuliia Shliapkina, Mariia Kaidash, Mariia Shyshkina, Svitlana Shishkina, Vladimir Musatov, Sergey Desenko, Valentyn Chebanov   +9 more
doaj   +1 more source

Polyamide Backbone Modified Cell Targeting and Penetrating Peptides in Cancer Detection and Treatment

Frontiers in Chemistry, 2020
Cell penetrating and targeting peptides (CPPs and CTPs) encompass an important class of biochemically active peptides owning the capabilities of targeting and translocating within selected cell types.
Sunil S. Shah, Nelson Casanova, Gina Antuono, David Sabatino   +3 more
doaj   +1 more source

Multicomponent synthesis and photophysical study of novel α,β-unsaturated carbonyl depsipeptides and peptoids

Frontiers in Chemistry, 2023
Multicomponent reactions were performed to develop novel α,β-unsaturated carbonyl depsipeptides and peptoids incorporating various chromophores such as cinnamic, coumarin, and quinolines.
Ricelia González, Juliana Murillo-López, Walter Rabanal-León, Luis Prent-Peñaloza, Odette Concepción, Pedro Olivares, Yorley Duarte, Alexander F. de la Torre, Margarita Gutiérrez, Julio Caballero   +9 more
doaj   +1 more source

Synthesis of acylhydrazino-peptomers, a new class of peptidomimetics, by consecutive Ugi and hydrazino-Ugi reactions

Beilstein Journal of Organic Chemistry, 2016
Herein we describe a versatile approach for the synthesis of acylhydrazino-peptomers, a new class of peptidomimetics. The key idea in this approach is based on a simple route using a one-pot hydrazino-Ugi four-component reaction followed by a ...
Angélica de Fátima S. Barreto, Veronica Alves dos Santos, Carlos Kleber Z. Andrade   +2 more
doaj   +1 more source

Recent Advances in Amphipathic Peptidomimetics as Antimicrobial Agents to Combat Drug Resistance

Molecules
The development of antimicrobial drugs with novel structures and clear mechanisms of action that are active against drug-resistant bacteria has become an urgent need of safeguarding human health due to the rise of bacterial drug resistance. The discovery
Ma Su, Yongxiang Su
doaj   +1 more source

C-Terminal Extended Hexapeptides as Potent Inhibitors of the NS2B-NS3 Protease of the ZIKA Virus

Frontiers in Medicine, 2022
The Zika virus (ZIKV) protease is an attractive drug target for the design of novel inhibitors to control the ZIKV infection. As the protease substrate-binding site contains acidic residues, inhibitors with basic residues can be beneficial for the ...
Suyash Pant, Nihar R. Jena
doaj   +1 more source

Beyond Simple Mimicry: Next‐Generation Geometric Architectures and Future Paradigms in Small‐Molecule and Macrocyclic Peptidomimetics

Angewandte Chemie International Edition, EarlyView.
Peptide‐to‐Small Molecule Paradigm: Peptidomimetics have evolved from simple mimicry toward drug‐like scaffolds supported by increasing clinical successes. This Perspective highlights the geometric design principles—linear repetition, convergent fusion, and cyclization—defining the next‐generation peptidomimetic architectures capable of targeting ...
Jesang Lee, Sumin Son, Jeong Yeon Yoo, Ji Hyae Lee, Meehyun Chun, Seung Bum Park   +5 more
wiley   +1 more source

Direct conversion of peptides into diverse peptidomimetics using a transformer-based chemical language model

European Journal of Medicinal Chemistry Reports
The design of pharmaceutically relevant compounds that mimic bioactive peptides or secondary structure elements in proteins is an important task in medicinal chemistry. Over time, various chemical strategies have been developed to convert natural peptide
Atsushi Yoshimori, Jürgen Bajorath
doaj   +1 more source

Solid-Phase Synthesis of Amine/Carboxyl Substituted Prolines and Proline Homologues: Scope and Limitations

Molecules, 2016
A solid-phase procedure is used to synthesize racemic peptidomimetics based on the fundamental peptide unit. The peptidomimetics are constructed around proline or proline homologues variably substituted at the amine and carbonyl sites.
Ziniu Zhou, William L. Scott, Martin J. O’Donnell   +2 more
doaj   +1 more source