A series of twenty six new 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine analogues were synthesized by seven steps and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Among the tested compounds, 7j, 7p, and 7r exhibited moderate activity (MIC = 6.25 μg/mL) and compounds 7a, 7f, 7g, 7n and 7v exhibited good activity (MIC = 3.125 μg/mL), while 7h displayed excellent activity (MIC = 1.56 μg/mL) by inhibiting 99% growth of M. tuberculosis H37Rv strain. In addition, all the active compounds were subjected to cytotoxic studies against mouse macrophage (RAW264.7) cell lines and the selectivity index values for most of the compounds is >10 indicating suitability of compounds in an endeavour to attain lead molecule for further drug development.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.ejmech.2014.07.067 | DOI Listing |
BMC Complement Med Ther
January 2025
Department of Faculty of Health Sciences, American University of Madaba, Madaba, Jordan.
Pseudomonas aeruginosa is an opportunistic pathogen belonging to the γ-proteobacteria family, known to cause pneumonia linked with ventilator use and nosocomial infections. With the increasing prevalence of antibiotic-resistant bacteria, there is a pressing need to identify alternatives to conventional antibiotics. Plant-derived substances (PDSs) offer potential not only as antibacterial agents but also as modulators of antibiotic resistance.
View Article and Find Full Text PDFCurr Microbiol
January 2025
Department of Microbiology and Immunology, School of Medicine, Soonchunhyang University, Cheonan-si, Chungnam, 31151, Republic of Korea.
Lactic acid bacteria (LAB), traditionally consumed as fermented foods, are now being applied to the medical field beyond health-functional food as probiotics. Therefore, it is necessary to continuously discover and evaluate new strains with suitable probiotic characteristics, mainly focusing on safety. In this study, we isolated eight new strains from postmenopausal vaginal fluid using culturomics approaches, an emerging area of interest.
View Article and Find Full Text PDFBiochim Biophys Acta Biomembr
January 2025
Biochemistry and Molecular Biology Department, Center for Pharmaceutical Research and Development, Ave. 26 # 1605, Nuevo Vedado, Ciudad de La Habana, 10400, Cuba. Electronic address:
Acylation is a common method used to modify antimicrobial peptides to enhance their effectiveness. It increases the interactions between the peptide and the bacterial cell membranes. However, acylation can also reduce the selectivity of the peptides by making them more active on eukaryotic membranes, which can lead to unintended toxicity.
View Article and Find Full Text PDFLife Sci
January 2025
Department of Rheumatism and Immunology, Peking University Shenzhen Hospital, Shenzhen 518036, China. Electronic address:
Pelophylax nigromaculata, common traditional Chinese medicinal material used for several hundreds of years, is one of the most widely distributed amphibians in China. In this study, a novel Ranatuerin-2 family antimicrobial peptide, Rana-2PN, was identified and characterized from its skin, and its structural characteristics and functional activities were studied extensively. First, Rana-2PN exhibited a broad spectrum of antimicrobial activity, displaying minimum inhibitory concentration (MIC) values ranging from 12.
View Article and Find Full Text PDFJ Asian Nat Prod Res
January 2025
Department of Molecular Biology and Genetics, Faculty of Science, Sivas Cumhuriyet University, Sivas, Turkey.
Antimicrobial peptides are crucial components of the immune systems of both vertebrates and invertebrates. Here, defensins, the most studied class of antimicrobial molecules in arthropods were investigated in four coleopteran insect species: (DeGeer, 1774), (Linnaeus, 1767), (Linnaeus, 1758), and (Brullé, 1832). The peptides synthesized with over 95% purity and their antimicrobial activities were evaluated by MIC test method.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!