Six griseofulvin analogues named penigriseofulvins A - F (1-6), including three undescribed compounds and three undescribed natural products, were isolated from the fungus Penicillium griseofulvum. Their structures and absolute configurations were determined by NMR spectroscopic analyses, HRESIMS, and X-ray diffraction experiments. All compounds were evaluated for their anti-inflammatory activity, of which compounds 1 and 4 showed potential anti-inflammatory effects in RAW264.7 macrophages and ulcerative colitis mice.
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http://dx.doi.org/10.1016/j.bioorg.2023.106736 | DOI Listing |
Int J Pharm
December 2024
New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ 07102, USA. Electronic address:
The downstream processability of Hot Melt Extrusion (HME) Amorphous Solid Dispersions (ASD), an underexplored topic of importance, was assessed through a multi-faceted particle engineering approach. Extrudates, comprised of griseofulvin (GF), a model poorly water-soluble drug, and hydroxypropyl cellulose (HPC), were prepared at four drug concentrations and three HME temperature profiles to yield cases with and without residual crystallinity and subsequently milled to five sieve cuts ranging from < 45 μm to 355 - 500 μm. Solid state characterization was performed with XRPD, FT-IR, and TGA.
View Article and Find Full Text PDFInt J Pharm
December 2024
Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 544 54 Thessaloniki, Greece. Electronic address:
Chem Biodivers
January 2025
Photochemistry Department, Chemical Industries Research Institute, National Research Centre, Scopus affiliation ID 60014618, 33 EL Buhouth St., Dokki, Giza, 12622, Egypt.
Herein, a one-pot reaction between cyclohexanone, thiourea, and 2,5-dimethoxybenzaldehyde allowed to prepare hexahydroquinazoline-2(1H)-thione4 firstly, which followed by reacting with hydrazine hydrate to produce the corresponding 2-hydrazinylhexahydroquinazoline 6. Interesting analogs of thiazolo[3,2-a]quinazoline 713 where obtained when hexahydroquinazoline-2(1H)-thione 4 reacted with 1,2-dibromoethane, chloroacetyl chloride, bromoacetic acid, bromoacetic acid/4-chlorobenzaldehyde, 2-bromopropionic acid, ethyl bromo cyanoacetate, and/or bromomalononitrile; respectively. While triazolo[4,3-a] quinazoline 14-16 were created when 2-hydrazinylhexahydroquinazoline 6 reacted with triethyl orthoformate, acetic anhydride, and carbon disulfide respectively.
View Article and Find Full Text PDFInt J Biol Macromol
September 2024
Department of Pharmaceutical Technology, Jadavpur University, Kolkata, 700032, India. Electronic address:
Fungal infections are very alarming nowadays and are common throughout the world. Severe fungal infections may lead to a significant risk of mortality and morbidity worldwide. Sustained delivery of antifungal agents is needed to mitigate this problem.
View Article and Find Full Text PDFMycopathologia
March 2024
Mycology and Aerobiology Department, Sciensano, 1050, Brussels, Belgium.
The emerging pathogen Trichophyton indotineae, often resistant to terbinafine (TRB), is known to cause severe dermatophytoses such as tinea corporis and tinea cruris. In order to achieve successful treatment for these infections, insight in the resistance profile of T. indotineae strains and rapid, reliable identification is necessary.
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