Original results are presented in the field of research that addresses the extension of the reaction of residue of acyl-thiosemicarbazide fixation on the structure of 5-nitrobenzimidazole by a sulphonic group. The aim of the study is the increase of new thiosemicarbazide derivatives' applicative potential in the field of biochemistry, with a wide range of medical applications. The newly obtained compounds were characterized by using elemental analysis and spectral analysis (FT-IR and H NMR). A study regarding the optimization of the chemical reactions was made. The performed in vitro biological tests confirmed the tuberculostatic activity of three newly obtained compounds against .
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http://dx.doi.org/10.3390/ijms222212139 | DOI Listing |
Cureus
November 2024
Plastic and Reconstructive Surgery, Hospital de Santa Maria, Unidade Local de Saúde Santa Maria (ULSSM), Lisbon, PRT.
Tuberculosis (TB) dactylitis of the hand is a rare and challenging pathology, requiring positive bacterial identification through culture or biopsy for diagnosis. Treatment is also challenging, although it typically yields an excellent response to long-term tuberculostatic therapy. We describe a case of osteoarticular tuberculous dactylitis in a 36-year-old woman with rheumatoid arthritis (RA) and a history of lymphoma.
View Article and Find Full Text PDFAntibiotics (Basel)
February 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, Traian Vuia no. 6, 020956 Bucharest, Romania.
N-acyl hydrazone (NAH) is recognized as a promising framework in drug design due to its versatility, straightforward synthesis, and attractive range of biological activities, including antimicrobial, antitumoral, analgesic, and anti-inflammatory properties. In the global context of increasing resistance of pathogenic bacteria to antibiotics, NAHs represent potential solutions for developing improved treatment alternatives. Therefore, this research introduces six novel derivatives of ()-N'-benzylidene-2-(6-chloro-9-carbazol-2-yl)propanehydrazide, synthesized using a microwave-assisted method.
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September 2023
Chair and Department of Biochemistry, The Medical University of Warsaw, 02-097, Warsaw, Poland.
In this work, we investigated the antitubercular properties of Ciprofloxacin derivatives conjugated with menthol and thymol moieties. For the sixteen derivatives, we established minimal inhibitory concentrations (MIC) using isolates of Mycobacterium tuberculosis that were resistant or susceptible to other antibiotics. For the most potent compound 1-cyclopropyl-6-fluoro-7-{4-[6-((1R,2S,5R)-2-isopropyl-5-methylcyclohexyloxy)-6-oxohexyl]piperazin-1-yl}-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (6), we determined fractional inhibitory concentration index (FICI) values to confirm antibacterial susceptibility and synergistic effects with other reference drugs.
View Article and Find Full Text PDFPharmaceuticals (Basel)
September 2023
Sunny BioDiscovery Inc., 972 East Main Str., Santa Paula, CA 93060, USA.
To investigate how structural modifications affect tuberculostatic potency, we synthesized seven new piperidinothiosemicrabazone derivatives -, in which three of them had a pyrazine ring replacing the pyridine ring. Derivatives - and - exhibited significant activity against the standard strain (minimum inhibitory concentration (MIC) 2-4 μg/mL) and even greater activity against the resistant strain (MIC 0.5-4 μg/mL).
View Article and Find Full Text PDFACS Omega
May 2023
Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland.
A novel series of N-acylated ciprofloxacin (CP) conjugates were synthesized and screened as potential antimicrobial agents. Conjugates and were 1.25-10-fold more potent than CP toward all (minimal inhibitory concentration 0.
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