Publications by authors named "I Agostino"
2,2'-Thio-bis(4,6-dichlorophenol), namely bithionol, is a small molecule endowed with a multifaceted bioactivity. Its peculiar polychlorinated phenolic structure makes it a suitable candidate to explore its potentialities in establishing interaction patterns with enzymes of MedChem interest, such as the human carbonic anhydrase (hCA) metalloenzymes. Herein, bithionol was tested on a panel of specific hCAs through the stopped-flow technique, showing a promising micromolar inhibitory activity for the hCA II isoform.
View Article and Find Full Text PDFPCI-27483, originally developed as a potent and selective inhibitor of the serine protease Factor VIIa (FVIIa) in complex with tissue factor (TF), has demonstrated significant promise in cancer therapy. In addition to its primary mechanism of action, the presence of a sulfonamide moiety in the PCI-27483 structure suggests further activities through the inhibition of carbonic anhydrases (CAs), particularly the tumor-associated human (h)CA isoforms hCA IX and XII. This study investigates the inhibitory activity of PCI-27483 against the complete panel of active hCAs, highlighting its polypharmacological potential in cancer treatment.
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- Nearly half of the global population is affected by an infection, with current treatments involving antibiotics and proton pump inhibitors; however, rising antimicrobial resistance remains a major issue.
- Phenolic monoterpenes like eugenol, vanillin, carvacrol, and thymol are of interest for their biological activities and potential for easy modifications, leading to the creation of mono- and bis-azo derivatives through aryl diazotization.
- The synthesized compounds were tested against various bacterial strains, revealing some effective inhibitors and subsequently underwent cytotoxicity evaluations and target investigations using structure-based docking calculations on key pharmacological targets.
Ciprofloxacin (CPX) is one of the most employed antibiotics in clinics to date. However, the rise of drug-resistant bacteria is dramatically impairing its efficacy, especially against life-threatening pathogens, such as . This Gram-negative bacterium is an opportunistic pathogen, often infecting immuno-compromised patients with severe or fatal outcomes.
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- - Lasamide, a synthetic byproduct of the diuretic Furosemide manufacturing, is highlighted as a valuable component for drug discovery techniques.
- - Researchers tested Lasamide's effectiveness in inhibiting human Carbonic Anhydrases (hCAs) using a stopped-flow method and examined its binding through X-ray crystallography.
- - The study introduces a new crystal form for a specific Carbonic Anhydrase mimic (hCA IX), which is discussed in detail.