We have synthesized new series of bisindole analogs (-), characterized by HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with standard pentamidine with IC value of 7.20 ± 0.20 µM. All analogs showed greater potential than standard except , and when compared with standard. Structure activity relationship has been also established for all compounds. Molecular docking studies were carried out to understand the binding interaction of active molecules.
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http://dx.doi.org/10.1186/s13065-019-0617-4 | DOI Listing |
ACS Biomater Sci Eng
January 2025
Department of Physiology, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, P.R. China.
Mitochondrial dysfunction contributes to the pathology of hypoxia-ischemia (HI) brain damage by aberrant production of ROS. Hydrogen sulfide (HS) has been demonstrated to exert neuroprotective effects through antioxidant mechanisms. However, the diffusion of HS is not specifically targeted and may even be systemically toxic.
View Article and Find Full Text PDFBioconjug Chem
January 2025
Department of Biotechnology and Bioengineering, Institute of Advanced Research, Gandhinagar 382426, India.
This work describes the synthesis, characterization, and antibacterial properties of four bile acid-triclosan conjugates. The in vitro antibacterial activity of synthetic bile acid-triclosan conjugates was investigated against a panel of Gram-positive and Gram-negative bacteria. Conjugates and show high activity against (ATCC25922), with IC values of 2.
View Article and Find Full Text PDFMinerva Dent Oral Sci
January 2025
Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences (SIMATS), Saveetha University, Chennai, India.
Background: Boswellic acid (BA) is a bioactive compound derived from Boswellia trees. This study aims to investigate the anti-cancer properties of BA against KB oral squamous cancer cells and elucidate the underlying mechanisms.
Methods: Escalating doses of BA were administered to KB cells, and various analyses were conducted using bioinformatic tools such as GEO, GEO2R, and STITCH database.
Mol Divers
January 2025
Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
The drug combination is an attractive approach for cancer treatment. PARP and kinase inhibitors have recently been explored against cancer cells, but their combination has not been investigated comprehensively. In this study, we used various drug combination databases to build ML models for drug combinations against brain cancer cells.
View Article and Find Full Text PDFMol Divers
January 2025
State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals, Guizhou University, Guiyang, 550025, China.
A series of flavonoid derivatives containing piperazine sulfonate were designed and synthesized. The results of antiviral experiments in vivo showed that some target compounds had good inhibitory effect on tobacco mosaic virus (TMV). The EC values of S15 and S19 curative activity were 174.
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