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Synthesis, larvicidal efficiency and molecular docking studies of novel annulated pyrano[2,3-c]pyrazoles against Culex pipiens L. and Musca domestica L. larvae

期刊: BIOORGANIC CHEMISTRY, 2023; 130 ()

A number of novel annulated pyrazolopyranopyrimidines were prepared via reaction of iminoether of the corresponding 6-amino-5-cyano-pyrano[2,3-c]pyraz......

Synthesis and structure-activity relationships of ticlopidine derivatives and analogs as inhibitors of ectonucleotidase CD39

期刊: BIOORGANIC CHEMISTRY, 2023; 135 ()

Ticlopidine is an antithrombotic prodrug of the thienotetrahydropyridine family. For platelet inhibition it has to undergo oxidative ring-opening by c......

Novel scaffolds targeting Mycobacterium tuberculosis plasma membrane Ca2+transporter CtpF by structure-based strategy

期刊: BIOORGANIC CHEMISTRY, 2023; 138 ()

CtpF is a Ca2+ transporter P-type ATPase key to the response to stress conditions and to Mycobacterium tuber-culosis virulence, therefore, an interest......

Recent developments in the synthesis of hybrid antimalarial drug discovery

期刊: BIOORGANIC CHEMISTRY, 2023; 139 ()

In this 21st century, Malaria remains a global burden and causes massive economic trouble to disease-endemic nations. The control and eradication of m......

Molecular imaging of tumor hypoxia: Evolution of nitroimidazole radiopharmaceuticals and insights for future development

期刊: BIOORGANIC CHEMISTRY, 2023; 139 ()

Though growing evidence has been collected in support of the concept of dose escalation based on the molecular level images indicating hypoxic tumor s......

Calix[4]arene-pyrazole conjugates as potential cancer therapeutics

期刊: BIOORGANIC CHEMISTRY, 2023; 139 ()

Tumor selectivity is yet a challenge in chemotherapy-based cancer treatment. A series of calixarenes derivatized at the lower rim with 3-phenyl-1H-pyr......

Introduction of constrained Trp analogs in RW9 modulates structure and partition in membrane models

期刊: BIOORGANIC CHEMISTRY, 2023; 139 ()

Over the past decades, many cell-penetrating peptides (CPP) have been studied for their capacity to cross cellular membranes, mostly in order to impro......

Synthesis and in vitro cytotoxic activity of dye-linker-macrocycle conjugates with variable linker length and components

期刊: BIOORGANIC CHEMISTRY, 2023; 140 ()

The study investigated the structure-activity relationship of newly synthesized dye-linker-macrocycle (DLM) conjugates and the effect of each componen......

Potential natural product 3,4-seco-schitriterpenoids from Kadsura japonica L. as anti-neuroinflammatory agents

期刊: BIOORGANIC CHEMISTRY, 2023; 141 ()

In the present study, the undescribed schitriterpenoids, kadsujanonols A-I (1-9), and eleven reported compounds (10-20) were isolated from K. japonica......

Synthesis and chemical transformations of glycol nucleic acid (GNA) nucleosides

期刊: BIOORGANIC CHEMISTRY, 2023; 141 ()

Xeno nucleic acids (XNA) are an increasingly important class of hypermodified nucleic acids with great potential in bioorganic chemistry and synthetic......

Modulating the affinity and signaling bias of cannabinoid receptor 1 antagonists

期刊: BIOORGANIC CHEMISTRY, 2023; 130 ()

Cannabinoid receptor 1 (CB1) is a G protein-coupled receptor and a therapeutic target for metabolic disorders. Numerous CB1 antagonists have been deve......

Phosphine chalcogenides and their derivatives from red phosphorus and functionalized pyridines, imidazoles, pyrazoles and their antimicrobial and cytostatic activity

期刊: BIOORGANIC CHEMISTRY, 2023; 132 ()

Tertiary phosphine oxides, phosphine sulfides, and phosphine selenides containing pyridine, imidazole, and pyrazole groups have been synthesized via t......

Biotinylated selenocyanates: Potent and selective cytostatic agents

期刊: BIOORGANIC CHEMISTRY, 2023; 133 ()

Most of the currently available cytotoxic agents for tackling cancer are devoid of selectivity, thus causing severe side-effects. This situation stimu......

tLyp-1: A peptide suitable to target NRP-1 receptor

期刊: BIOORGANIC CHEMISTRY, 2023; 130 ()

Targeting vascular endothelial growth factor receptor (VEFGR) and its co-receptor neuropilin-1 (NRP-1) is an interesting vascular strategy. tLyp-1 is ......

Exploring the dual effect of novel 1,4-diarylpyranopyrazoles as antiviral and anti-inflammatory for the management of SARS-CoV-2 and associated inflammatory symptoms

期刊: BIOORGANIC CHEMISTRY, 2023; 130 ()

COVID-19 and associated substantial inflammations continue to threaten humankind triggering death world-wide. So, the development of new effective ant......

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