Results 21 to 30 of about 17,763 (235)

Antibiotic Potentiation in Multidrug-Resistant Gram-Negative Pathogenic Bacteria by a Synthetic Peptidomimetic.

open access: yesACS Infectious Diseases, 2021
The peptidomimetic H-[NLys-tBuAla]6-NH2 (CEP-136), which exhibits low inherent antimicrobial activity against Gram-negative bacteria (MIC = 16-64 μM), was shown to significantly potentiate the antibacterial activity of several clinically important ...
Elnaz Harifi Mood   +8 more
semanticscholar   +1 more source

Brilacidin Demonstrates Inhibition of SARS-CoV-2 in Cell Culture

open access: yesViruses, 2021
Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the newly emergent causative agent of coronavirus disease-19 (COVID-19), has resulted in more than two million deaths worldwide since it was first detected in 2019.
Allison Bakovic   +7 more
doaj   +1 more source

Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.

open access: yesRSC Medicinal Chemistry, 2021
Tragically, the death toll from the COVID-19 pandemic continues to rise, and with variants being observed around the globe new therapeutics, particularly direct-acting antivirals that are easily administered, are desperately needed. Studies targeting the
Bing Bai   +16 more
semanticscholar   +1 more source

Copper chelating cyclic peptidomimetic inhibits Aβ fibrillogenesis.

open access: yesRSC Medicinal Chemistry, 2022
Misfolding of the amyloid-β peptide (Aβ) and its subsequent aggregation into toxic oligomers is one of the leading causes of Alzheimer's disease (AD). As a therapeutic approach, cyclic peptides have been modified in many ways and developed as a potential
S. Kalita   +6 more
semanticscholar   +1 more source

A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors

open access: yesBioorganic & Medicinal Chemistry Letters, 2021
The COVID-19 pandemic caused by SARS-CoV-2 has created an unprecedented global health emergency. As of July 2021, only three antiviral therapies have been approved by the FDA for treating infected patients, highlighting the urgent need for more ...

semanticscholar   +1 more source

Synthesis of imidazo[1,2-a]pyridine-containing peptidomimetics by tandem of Groebke–Blackburn–Bienaymé and Ugi reactions

open access: yesBeilstein Journal of Organic Chemistry, 2023
Peptidomimetics with a substituted imidazo[1,2-a]pyridine fragment were synthesized by a tandem of Groebke–Blackburn–Bienaymé and Ugi reactions. The target products contain substituted imidazo[1,2-a]pyridine and peptidomimetic moieties as pharmacophores ...
Oleksandr V. Kolomiiets   +5 more
doaj   +1 more source

QSAR Modelling of Peptidomimetic Derivatives towards HKU4-CoV 3CLpro Inhibitors against MERS-CoV

open access: yesChemistry, 2021
In this paper, we report the relationship between the anti-MERS-CoV activities of the HKU4 derived peptides for some peptidomimetic compounds and various descriptors using the quantitative structure activity relationships (QSAR) methods.
Imad Hammoudan   +4 more
doaj   +1 more source

A pH-sensitive liposome formulation of a peptidomimetic-Dox conjugate for targeting HER2 + cancer

open access: yesInternational journal of pharmaceutics, 2021
Cancer treatment faces the challenge of selective delivery of the cytotoxic drug to the desired site of action to minimize undesired side effects.
Jafrin Jobayer Sonju   +7 more
semanticscholar   +1 more source

1,2,3-Triazoles as Biomimetics in Peptide Science

open access: yesMolecules, 2021
Natural peptides are an important class of chemical mediators, essential for most vital processes. What limits the potential of the use of peptides as drugs is their low bioavailability and enzymatic degradation in vivo.
Naima Agouram   +2 more
doaj   +1 more source

A VEGFB-Based Peptidomimetic Inhibits VEGFR2-Mediated PI3K/Akt/mTOR and PLCγ/ERK Signaling and Elicits Apoptotic, Antiangiogenic, and Antitumor Activities

open access: yesPharmaceuticals, 2023
Vascular endothelial growth factor receptor 2 (VEGFR2) mediates VEGFA signaling mainly through the PI3K/AKT/mTOR and PLCγ/ERK1/2 pathways. Here we unveil a peptidomimetic (VGB3) based on the interaction between VEGFB and VEGFR1 that unexpectedly binds ...
Mohadeseh Namjoo   +8 more
doaj   +1 more source

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