A diverse range of 9-substituted 1,8-dioxohexahydroxanthenes was conceptualized and synthesized through a TFA-mediated approach in near quantitative yields without the use of column chromatography. From a series of 25 compounds, we found that compounds 14c and 14r exhibited promising anti-tuberculosis potential against avirulent and virulent strains of with a Minimal Inhibitory Concentration (MIC) of 8 μg ml, achieving 99% bactericidal activity at the same concentration. This series of compounds was found to be inactive against common Gram-positive and Gram-negative pathogens, indicating that the activity is mycobacteria-specific. Since the strategies for treating tuberculosis employ a combinatorial therapy, we tested and observed that the two lead compounds displayed synergistic behavior with known anti-TB drugs (ATDs) and a significant (16-32 fold) decrease in MIC values of both leads was observed in combination with either RIF or INH. Interestingly the lead molecule 14c displayed only time-dependent kill kinetics and sterilized the whole culture of H37Rv in just 48 hours.
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http://dx.doi.org/10.1039/d3md00518f | DOI Listing |
Sci Rep
January 2025
Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
A series of novel phenylamino quinazolinone derivatives were designed and synthesized as potential tyrosinase inhibitors. Among these compounds, 9r emerged as the most potent derivative, exhibiting IC values of 17.02 ± 1.
View Article and Find Full Text PDFBioorg Chem
December 2024
Universidade da Coruña, CICA - Centro Interdisciplinar de Química e Bioloxía and Departamento de Química, Facultad de Ciencias, Campus A Zapateira, 15071 A Coruña, Spain. Electronic address:
In this study, a series of BODIPY dyes were synthesized, containing various substituents at meso position. Further functionalization of the BODIPY framework at C2 and C2-C6 position(s) by palladium-catalysed cross-coupling reactions using organoindium reagents (RIn) was efficiently assessed, starting from C2(6)-halogenated BODIPYs, and their optical properties were measured. The cytotoxicity of BODIPY dyes on SH-SY5Y neuronal cells by MTT assay showed that those compounds bearing thien-2-yl and benzonitrile moieties at meso position, exhibited great efficiency in maintaining cell viability under all tested conditions (up to 50 µM for 24 h and 48 h).
View Article and Find Full Text PDFBioorg Chem
December 2024
Pharmacology Division, CSIR- Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Ursolic acid (3-hydroxy-urs-12-ene-28-oic acid, UA) is a pentacyclic triterpene present in numerous plants, fruits and herbs and exhibits various pharmacological effects. However, UA has limited clinical applicability since it is classified as BCS class IV molecule, characterized by low solubility, low oral bioavailability and low permeability. In the present study, UA was isolated from the biomass marc of Lavandula angustifolia and was structurally modified by an induction of indole ring at the C-3 position and amide group at the C-17 position with the aim to enhance its pharmacological potential.
View Article and Find Full Text PDFAnal Chem
January 2025
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
Quaternary ammonium salts (QAs) are a class of highly active compounds widely used in medicine and agriculture. However, many QAs lack a conjugated system, making their recognition and quantitation challenging. Stachydrine is a representative unconjugated QA with a high content in Houtt.
View Article and Find Full Text PDFCurr Nutr Rep
January 2025
Institute of Nutrition, Mahidol University, 999 Phutthamonthon 4 Road, Nakhon Pathom, 73170, Salaya, Thailand.
Purpose Of Review: The diverse polyphenolic components present in these berries are responsible for their functional properties in human health. Hence, there is an increasing demand for research in berry bioactive components to understand the mechanism of action in alleviating and preventing diseases. Therefore, in this last part-III of the review series, mulberry, raspberry, salmonberry, Saskatoonberry, and strawberry are discussed in terms of their bioactive components and corresponding substantial health benefits.
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