Expanding the Chemical Space of Reverse Fosmidomycin Analogs.

Multidrug-resistant pathogens pose a major threat to human health, necessitating the identification of new drug targets and lead compounds that are not susceptible to cross-resistance. This study demonstrates that novel reverse thia analogs of the phosphonohydroxamic acid antibiotic fosmidomycin inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), an essential enzyme for , , and that is absent in humans. Some novel analogs with large α-phenyl substituents exhibited strong inhibition across these three DXR orthologues, surpassing the inhibitory activity of fosmidomycin.

The influence of serum uric acid on coronary atherosclerosis plaque phenotypes by computed tomography angiography: The missing link?

Background And Aims: The interaction of serum uric acid (SUA) with atherogenesis is incompletely understood. Aim of our study was to investigate the association of SUA levels with coronary plaque composition including high-risk-plaque (HRP) features by coronary computed tomography angiography (CTA) and for the prediction of major adverse cardiac events (MACE).

Methods And Results: 1242 patients (age 66.

Towards Novel Antiplasmodial Agents-Design, Synthesis and Antimalarial Activity of Second-Generation β-Carboline/Chloroquine Hybrids.

As the resistance of to the existing antimalarials increases, there is a crucial need to expand the antimalarial drug pipeline. We recently identified potent antimalarial compounds, namely harmiquins, hybrids derived from the β-carboline alkaloid harmine and 4-amino-7-chloroquinoline, a key structural motif of chloroquine (CQ). To further explore the structure-activity relationship, we synthesised 13 novel hybrid compounds at the position -9 of the β-carboline ring and evaluated their efficacy in vitro against 3D7 and Dd2 strains (CQ sensitive and multi-drug resistant, respectively).

Diagnostic Impact of Subcutaneous Edema in Gouty Feet Detected by Dual-Energy Computed Tomography and Ultrasound.

: The objective of our study was to evaluate the association and frequency of subcutaneous lymphedema in patients with gout primarily affecting the feet. : In 79 patients with acute gout, ultrasound (US) and dual-energy computed tomography (DECT) were performed to assess the presence of subcutaneous edema and extra- and intra-articular gouty deposits. In addition, the diagnostic utility of two post-processing DECT protocols were evaluated, comprising different minimum attenuation thresholds of 150 HU (DECT 150 protocol) and 120 HU (DECT 120 protocol), with the same maximum attenuation threshold (500 HU) and constant kilovoltage setting of tubes A and B at 80 and 140 kVp.

TKK130 is a 3-Hydroxy-Propanamidine (HPA) with Potent Antimalarial Activity and a High Barrier to Resistance.

Malaria continues to pose a significant burden on populations in endemic areas and requires innovative treatment options. Here, we report the synthesis and preclinical evaluation of the novel 3-hydroxypropanamidine (HPA) , which shows excellent antiplasmodial activity against drug-sensitive and -resistant strains. Moreover, in various human cell lines, the compound shows no cytotoxicity and excellent parasite selectivity.