Search
Search Results
-
The kappa-opioid receptor agonist, triazole 1.1, reduces oxycodone self-administration and enhances oxycodone-induced thermal antinociception in male rats
RationaleTriazole 1.1 is a novel kappa-opioid receptor (KOR) agonist reported to produce antinociception without KOR-typical adverse effects. When...
-
Pharmacophore variants of the macrocyclic peptide triazole inactivator of HIV-1 Env
Previously we established a family of macrocyclic peptide triazoles (cPTs) that inactivate the Env protein complex of HIV-1, and identified the...
-
1,4-Diaryl-1,2,3-triazole neolignan–celecoxib hybrids inhibit experimental arthritis induced by zymosan
Rheumatoid arthritis (RA) is a chronic autoimmune disease that causes cartilage damage. Anti-inflammatories are widely used in the management of RA,...
-
Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism. Here, we designed twenty new analogs to...
-
New purine-triazole hybrids as potential anti-breast cancer agents: synthesis, antiproliferative activity, and ADMET in silico study
Two series of new 1,2,3-triazole-purine hybrids were synthesized in considerable yields (up to 87%), starting from benzyl azides and purine alkynes,...
-
A Poly(carbazole-alt-triazole) with Thiabendazole Side Groups as an “On-Off-On” Fluorescent Probe for Detection of Cu(II) Ion and Cysteine
A novel conjugated polymer PCZBTA-TBZ containing thiabendazole as recognition unit was synthesized via Suzuki coupling reaction, and its structural...
-
Contingent administration of typical and biased kappa opioid agonists reduces cocaine and oxycodone choice in a drug vs. food choice procedure in male rhesus monkeys
RationaleCombinations of mu and kappa-opioid receptor (KOR) agonists have been proposed as analgesic formulations with reduced abuse potential. The...
-
Synthesis, in-silico based virtual screening,anti-cancer potential of novel1,2,3-triazole-thiadiazole hybrid derivatives as Aurora kinase A (ARK-A) and Extracellular regulated kinase 2 (ERK2) dual inhibitors
As part of our ongoing efforts to produce promising cytotoxic agents, the novel compounds, 5-(4-(diethylamino)-2-((1-substitutedphenyl-1 H -1,2,3-triazo...
-
Altered Env conformational dynamics as a mechanism of resistance to peptide-triazole HIV-1 inactivators
BackgroundWe previously developed drug-like peptide triazoles (PTs) that target HIV-1 Envelope (Env) gp120, potently inhibit viral entry, and...
-
Pharmacokinetics and biodistribution of a novel anticancer thyrointegrin αvβ3 antagonist: triazole modified tetraiodothyroacetic acid conjugated to polyethylene glycol (P-bi-TAT)
AbstractWe previously developed a triazole modified tetraiodothyroacetic acid (TAT) conjugated to a polyethylene glycol (PEG)-based thyrointegrin...
-
Syntheses and anticancer activities of novel glucosylated (−)-epigallocatechin-3-gallate derivatives linked via triazole rings
Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogs conjugated to the d -glucosyl azide were synthesized by...
-
Recent pharmacological insights about imidazole hybrids: a comprehensive review
In this review, we evaluated the biological activities of hybrid molecules incorporating imidazoles—a cornerstone in medicinal chemistry known for...
-
New phthalimide-benzamide-1,2,3-triazole hybrids; design, synthesis, α-glucosidase inhibition assay, and docking study
A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a–k as α -glucosidase inhibitors was designed and synthesized. The biological evaluation...
-
A Click Synthesis, Molecular Docking and Biological Evaluation of 1,2,3-triazoles-benzoxazepine hybrid as potential anticancer agents
A series of novel 1,2,3-triazole-benzoxazepine hybrid molecules were synthesized and evaluated for their anticancer properties against four cancer...
-
Semi-synthesis of novel thebaine derivatives with low cytotoxicity and their antibacterial and antihemolytic properties
In the present study, some new 1,2,3-triazole-tethered analogs of N -northebaine were designed and synthesized. The anti-bacterial properties of novel...
-
New acridine-9-carboxamide linked to 1,2,3-triazole-N-phenylacetamide derivatives as potent α-glucosidase inhibitors: design, synthesis, in vitro, and in silico biological evaluations
α-Glucosidase plays a major role in degradation of carbohydrates to glucose. Therefore, inhibition of this enzyme can be useful in the treatment of...
-
Luciferase-Based High-Throughput Screen with Aspergillus fumigatus to Identify Antifungal Small Molecules
Only three classes of contemporary antifungal drugs are routinely utilized in the clinic against filamentous fungal pathogens such as Aspergillus...
-
Merging antimicrobial and visible emission properties within 1,3,4-trisubstituted-1,2,3-triazolium salts
Bioactive molecules displaying visible wavelength emission can be useful for bioimaging, chemosensing and photodynamic therapy applications. Reported...
-
Quantification of observable behaviors induced by typical and atypical kappa-opioid receptor agonists in male rhesus monkeys
RationaleKappa-opioid receptor (KOR) agonists are antinociceptive but have side effects that limit their therapeutic utility. New KOR agonists have...
-
Mechanisms involved in the antinociceptive and anti-inflammatory effects of a new triazole derivative: 5-[1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole (LQFM-096)
The aim of this study was to design, synthesize and evaluate the potential analgesic and anti-inflammatory effects of...
