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Unlabelled: Background and Introduction: Mefloquine, a drug used to prevent and treat malaria is described possessing activity against the Mycobacterium tuberculosis (Mtb) as well as against multidrugresistant tuberculosis (MDR) and other types of bacteria. Despite their importance, few compounds based on the Mefloquine nucleus have been synthesized and evaluated against TB.
Materials And Methods: For the synthesis of all the compounds based on the Mefloquine nucleus we used a synthetic route which utilized the key derivative 4-methoxy-2,8-bis(trifluoromethyl)quinoline 2 as starting material. The compounds 3 (a-c), 4 (a-b) were synthesized after one step by reaction of 2 with appropriate amines substituted. The chloro derivatives 5 and 6 were obtained from compounds 4b and 4a by treatment with SOCl2 in CH2Cl2 at reflux in 75 and 80% yield, respectively. The analogue 6 was converted to 7 after treatment with ethanolamine under heating at 90oC in 64% yield and to the azido derivative 8 in 56% after reaction with sodium azide in MeOH at reflux for 2 h. The analogue 9 was obtained after reaction of 5 with ethanolamine at 90oC for 1 h in 90% yield. All the new compounds were identified by detailed spectral data, including 1H NMR, 13C NMR and high resolution mass spectra. All the compound were evaluated for their in vitro antibacterial activity against sensitive Mycobacterium tuberculosis ATCC 27294, using the microplate Alamar Blue assay (MABA). The more active compounds 3c, 7, and 9 were also evaluated against resistant strain SR 2571/0215 (resistant to Rifampicin and Isoniazid) by above method. All compounds were tested against three cancer cell lines: SF-295 (glioblastoma), HCT-116 (colon) and PC-3 (prostate) using the MTT assay.
Results: All the planned ten compounds were synthetically obtained in good global yield, displaying activity against sensitive Mycobacterium tuberculosis in vitro, with exception of one, with MIC values between 37.2 and 154.8 µM. The compounds 3c (37.2 µM), 7 (68.1 µM) and 9 (65.6 µM) showed the highest activity in this series with MIC values similar when compare to the standard Mefloquine (30 - 60 µM), being 3c the most potent. The more active compounds 3c, 7, and 9 were also evaluated against resistant strain, displaying MIC of 37.2, 136.2 and 65.6 µM, respectively. All compounds were tested against three cancer cell lines and showed low cytotoxicity.
Conclusion: All synthesized compounds, with the exception of 5, exhibited activity against the Mtb. Compound 3c was the most potent against resistant and sensitive Mtb in this series, with MIC value of 37.2 µM. All compounds showed low cytotoxicity. These findings could be considered a good model to develop possible lead compounds in the fight against TB based on Mefloquine nucleus.
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http://dx.doi.org/10.2174/1568026619666190304124952 | DOI Listing |
Lett Appl Microbiol
December 2024
Amrita School for Nanosciences and Molecular Medicine, Amrita Vishwa Vidyapeetham, Kochi-682041, India.
Mycobacterium marinum is a slow growing Non-Tuberculosis Mycobacteria (NTM) known to cause skin and subcutaneous tissue infections known as "fish tank granuloma" in humans. Treatment of M. marinum skin infections can last for several months or even years.
View Article and Find Full Text PDFLung India
January 2025
Grupo de Bibliometría, Evaluación de Evidencia y Revisiones Sistemáticas (BEERS), Human Medicine Career, Universidad Científica del Sur, Lima, Peru, South America.
Background: Mycobacterium tuberculosis (M. tuberculosis) is an infectious disease that remains a significant global health problem. Despite efforts to reduce the disease, the disease remains prevalent in many parts of the world.
View Article and Find Full Text PDFJ Clin Invest
December 2024
Department of Molecular Immunology, Research Institute for Microbial Diseas, Osaka University, Suita, Japan.
Mycobacterium tuberculosis causes human tuberculosis. As mycobacteria are protected by thick lipid cell wall, humans have developed immune responses against diverse mycobacterial lipids. Most of these immunostimulatory lipids are known as adjuvants acting through innate immune receptors, such as C-type lectin receptors.
View Article and Find Full Text PDFInt J Mol Med
March 2025
Orthopedics of Chun'an First People's Hospital, Zhejiang Provincial People's Hospital Chun'an Branch, Affiliated Chun'an Hospital of Hangzhou Medical College, Hangzhou, Zhejiang 311700, P.R. China.
The world's leading infectious disease killer tuberculosis (TB) has >10 million new cases and ~1.5 million mortalities yearly. Effective TB control and management depends on accurate and timely diagnosis to improve treatment, curb transmission and reduce the burden on the medical system.
View Article and Find Full Text PDFIDCases
November 2024
Doctor of Medicine and Surgery, Hospital Escuela Universitario, Honduras.
Tuberculosis is a transmissible disease caused by the bacterium . It is the leading cause of mortality due to infectious diseases. Tuberculous pericarditis is one of the manifestations of extrapulmonary tuberculosis and represents the primary cause of pericardial effusion in developing countries.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!