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Several derivatives of aminobenzoboroxole have been prepared starting from 2-boronobenzaldehyde. All of these derivatives have been evaluated for their -mycobacterial activity on and cytotoxicity on breast cancer cell line MCF7. Based on these studies, all the tested molecules have been found to be generally non-toxic and benzoboroxoles with unsubstituted (primary) amines have been found to exhibit good -mycobacterial activity. Some of the key compounds have been evaluated for their -tubercular activity on H37Rv using 7H9 and GAST media. 7-Bromo-6-aminobenzoboroxole has been identified as the lead candidate compound for further development.
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http://dx.doi.org/10.1016/j.tet.2016.03.038 | DOI Listing |
Infect Immun
September 2025
School of Veterinary Medicine and Biomedical Sciences, University of Nebraska, Lincoln, Nebraska, USA.
Cell death mechanisms play a fundamental role in mycobacterial pathogenesis. We critically reviewed 94 research manuscripts, 44 review articles, and 4 book chapters to analyze important discoveries, background literature, and potential shortcomings in the field. The focus of this review is the pathogen (Mtb) and other Mtb and complex microorganisms.
View Article and Find Full Text PDFRSC Adv
August 2025
Department of Chemistry, Research Centre HPT Arts and RYK Science College (Affiliated to S. P. Pune University) Nashik Maharashtra 422005 India
The persistent threat of pathogenic microorganisms demands the development of innovative scaffolds with dual antibacterial and antifungal activities. Herein, we report the synthesis and characterization of a novel series of benzothiazole-thiazole hybrids (4a-4f) a three-step route, confirmed by NMR and MS analyses. The compounds were screened against Gram-positive, Gram-negative, mycobacterial, and fungal strains using disk diffusion and REMA assays.
View Article and Find Full Text PDFInt J Biol Macromol
September 2025
Department of Biomedical Science, Acharya Narendra Dev College, University of Delhi, Govindpuri, Kalkaji, 110019, New Delhi, India. Electronic address:
Mycobacteriophage-encoded LysinB enzymes target mycolyl ester linkages in mycolyl-arabinogalactan-peptidoglycan of mycobacterium hosts and generally exhibit a globular architecture. Here, we present the structural and functional characterization of a novel Mycobacterium fortuitum prophage-encoded modular LysinB (LysinB_MF), which contains the α/β hydrolase domain and a distinct peptidoglycan-binding domain (PGBD). The enzyme's active site features the conserved Ser-Asp-His catalytic triad common to esterases and forms a funnel-like topology.
View Article and Find Full Text PDFTuberculosis (Edinb)
August 2025
Mycobacteria Research, Bacterial and Parasite Disease Biology, Rajiv Gandhi Centre for Biotechnology, Thycaud P.O., Trivandrum, 695014, Kerala, India. Electronic address:
Mycobacterium tuberculosis (M. tuberculosis) persists within macrophages by evading phagosome maturation. In this study, we considered the role of actin dynamics in this process.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
September 2025
Department of Microbiology and Immunology, Albert Einstein College of Medicine, Bronx, NY 10461.
The ESX-5 secretion system, uniquely found in slow-growing mycobacteria, is predicted to secrete over 150 proteins across the inner membrane of (). Although many of these substrates are believed to promote virulence, most remain poorly characterized. Here, we use a complete locus deletion strain of ESX-5 in to examine the molecular changes caused by a broad loss in ESX-5 secretory substrates.
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