Guided by the metabolism information of SQ109, derivatives with substituted geranylamine moiety or substituted admantane ring of SQ109 were synthesized and evaluated as antituberculosis agents. Among all tested compounds, compound 11c showed the most potent antituberculosis activity with MIC value of 0.3 microM against Mycobacterium tuberculosis H37Rv.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2009.07.126 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Macrophage Activation Syndrome in a Patient with Systemic Lupus Erythematous Triggered by Tuberculous Meningitis.
Eur J Case Rep Intern Med
December 2024
Internal Medicine, Dubai Health, Dubai, United Arab Emirates.
Background: Hemophagocytic lymphohistiocytosis (HLH), is characterized by systemic uncontrolled inflammation resulting from immune dysregulation secondary to various triggers, including genetics, infections, autoimmune diseases, and malignancies. Macrophage activation syndrome (MAS) is an immune dysregulation phenomenon, in which an underlying rheumatological disease is present. We report a rare, interesting case of a middle-aged female, with a systemic lupus erythematosus (SLE) flare complicated by macrophage activation syndrome (MAS), in which tuberculous meningitis (TBM) was the identified trigger.
View Article and Find Full Text PDFNew Ionic Liquid Forms of Antituberculosis Drug Combinations for Optimized Stability and Dissolution.
AAPS PharmSciTech
January 2025
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Isoniazid (INH) and rifampicin (RIF) are the two main drugs used for the management of tuberculosis. They are often used as a fixed drug combination, but their delivery is challenged by suboptimal solubility and physical instability. This study explores the potential of active pharmaceutical ingredient-ionic liquids (API-ILs) to improve the physicochemical and pharmaceutical properties of INH and RIF.
View Article and Find Full Text PDFIdentification of novel 3-dehydroquinate dehydratase (DHQD) inhibitors for anti-tuberculosis activity: insights from virtual screening, molecular docking, and dynamics simulations.
In Silico Pharmacol
January 2025
Molecular Biophysics and Structural Biology (MBSB) Group, Department of Biochemistry, University of Johannesburg, Auckland Park Kingsway Campus, Johannesburg, 2006 South Africa.
Tuberculosis (TB) remains a pressing global health concern, causing substantial mortality and morbidity despite existing drugs and vaccines. The escalating challenge of drug-resistant TB underscores the critical need for novel medications. This study focuses on the enzyme 3-hydroquinate dehydratase (DHQD) in the shikimate pathway of (Mtb), essential for Mtb growth.
View Article and Find Full Text PDFEnhancing Antituberculosis Treatment Nanoparticles Encapsulated with Catalase and Levofloxacin Under Ultrasound Stimulation: A 3D Spheroid Study.
Mol Pharm
January 2025
State Key Laboratory of Ultrasound in Medicine and Engineering, College of Biomedical Engineering, Chongqing Medical University, Chongqing 400016, China.
Tuberculosis (TB) is a chronic infectious disease caused by (MTB). Tuberculous granuloma is the central and key pathological structure of tuberculosis and is characterized by tissue hypoxia and ineffective drug delivery. To address these issues, this study fabricated a composite nanoparticle loaded with catalase (CAT) and levofloxacin (LEV) (CAT@LEV-NPs) and then combined it with ultrasound (US) to investigate the bactericidal effect and underlying mechanisms using TB spheroids.
View Article and Find Full Text PDFDetection of Mycobacterium tuberculosis DNA in intraocular fluid of 11 suspected tuberculous uveitis patients by multiplex PCR.
BMC Ophthalmol
January 2025
Department of Tuberculosis, New District Branch of Northern Jiangsu People's Hospital of Jiangsu Province, Yangzhou, 225001, Jiangsu Province, China.
Background: This study aims to detect Mycobacterium tuberculosis complex (MTBC) DNA in intraocular fluid from clinically suspected tuberculous uveitis patients using multiplex polymerase chain reaction (PCR) and investigate the diagnostic utility of multiplex PCR for tuberculous uveitis.
Methods: Primers targeting three specific genes (MPB64, CYP141, and IS6110) within the MTBC genome were designed. Multiplex PCR was conducted using DNA from the H37Rv strain as well as DNA extracted from fluids of confirmed tuberculosis patients to assess primer specificity and method feasibility.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!