Synthesis, characterization, biological activities, and computational studies of pyrazolyl-thiazole derivatives of thiophene.

This study reports the synthesis, characterization, and biological evaluation of a series of pyrazolyl-thiazole derivatives of thiophene. Seven compounds were synthesized and characterized using NMR spectroscopy and mass spectrometry. The antimicrobial activities of these derivatives were evaluated against various bacterial (, , , ) and fungal strains (, , , ), demonstrating significant inhibition zones and low minimum inhibitory concentrations (MIC).

Imlunestrant is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wildtype and Mutant Breast Cancer.

Targeting of the estrogen receptor (ER) by anti-estrogens is the standard-of-care for patients with ER+ HER2- advanced/metastatic breast cancer. While anti-estrogens that degrade ERα (fulvestrant) or block estrogen production (aromatase inhibitors) have improved patient outcomes, clinically important challenges remain related to drug administration, limited bioavailability, lack of brain exposure, and acquired resistance due to ESR1 mutations. These limitations indicate a need for more robust ER-targeted therapies.

Fabrication of Microstructured Hydrogels via Dehydration for On-Demand Applications.

Microstructured hydrogels show promising applications in various engineering fields from micromolds to anisotropic wetting surfaces and microfluidics. Although methods like molding by, e.g.

Serum Pharmacokinetics and Bone Penetration of Novel Broad-Spectrum Anti-MRSA Agent Levonadifloxacin in Wistar Rats.

Levonadifloxacin (IV) and alalevonadifloxacin (oral) are novel broad-spectrum anti-methicillin-resistant () agents based on novel benzoquinolizine core. Both are recently approved in India for the treatment of acute bacterial skin and skin structure infections, including diabetic foot infections and concurrent bacteremia. The present investigation reports the findings from preclinical pharmacokinetic (PK) studies that support the development of levonadifloxacin as a treatment option for bone and joint infections (BJIs).