Mefloquine synergism with anti-tuberculosis drugs and correlation to membrane effects: Biologic, spectroscopic and molecular dynamics simulations studies

Santos, Marinalva Cardoso dos; Scaini, João L.; Lopes, Márcio Vinicius Costa; Rodrigues, Beatriz Gonçalves; Silva, Nichole Osti; Borges, Carla Roberta Lopes de Azambuja; Santos, Sandra Cruz dos; Machado, Karina; Werhli, Adriano Velasque; Silva, Pedro Eduardo Almeida da; Lourenço, Maria Cristina S.; Silva, Emerson T. da; Souza, Marcus V. N. de; Lima, Vânia Rodrigues de; Gonçalves, Rinaldo

doi:10.1016/j.bioorg.2021.104786

Cited by 8 publications

(9 citation statements)

References 67 publications

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“…e contribution of rural tourism to the local economy and the significance of local development have been well proven. In many countries, it is agreed that rural tourism is the driving force of economic development and economic diversification in remote rural areas [17,18].…”

Section: Network Informationization Of Rural Tourism Based On Mvc Modelmentioning

confidence: 99%

Design and Management of Control System for Rural Tourism Network Information Based on MVC Model

Dong

2021

Mobile Information Systems

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Tourism has developed into an industry with a powerful momentum of development in the world today. With the development of information technology, information has become a powerful driving force to promote the prosperity and development of the tourism industry and the entire society. The introduction of the tourism information system can significantly improve the service level, operation level, and management level of the tourism industry, thereby accelerating tourism development. The research of this article is to help villages establish a set of MVC-based rural tourism information service systems that can promote the development of rural tourism. First of all, this article conducts demand research on tourists, rural scenic spots, and ancient villages to discover the problems in rural tourism development. Secondly, this paper combines the problems existing in constructing the various subsystems of the rural tourism information system, combined with the fuzzy comprehensive evaluation method. In this paper, we propose the rural tourism system architecture based on MVC. The system architecture consists of the user layer, service layer, business layer, and data layer. It describes the system’s implementation process from two aspects: the system’s interface design and its deployment model. Finally, the network topology structure of the rural tourism information service system based on MVC is drawn. Finally, the system’s deployment is implemented according to the network topology structure.

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Section: Network Informationization Of Rural Tourism Based On Mvc Modelmentioning

confidence: 99%

Design and Management of Control System for Rural Tourism Network Information Based on MVC Model

Dong

2021

Mobile Information Systems

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“…Upon closer examination, these papers encompass a range of study types: there are 19 instances of in vitro research reported within these papers, of which five investigate synergistic effects specifically. Additionally, there are three instances of in vivo animal research and a single ongoing Phase 1 clinical trial retrieved from ClinicalTrials.Gov (Table 3, Additional file 1: Tables S3-S6) [26][27][28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44]. These studies, predominantly published between 2006 and 2021, with a peak from 2016 to 2019, explored anti-malarial drug activity against MTC.…”

Section: Resultsmentioning

confidence: 99%

Repurposing of anti-malarial drugs for the treatment of tuberculosis: realistic strategy or fanciful dead end?

Hanscheid,

del Portal Luyten,

Hermans

et al. 2024

Malar J

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Background Drug repurposing offers a strategic alternative to the development of novel compounds, leveraging the known safety and pharmacokinetic profiles of medications, such as linezolid and levofloxacin for tuberculosis (TB). Anti-malarial drugs, including quinolones and artemisinins, are already applied to other diseases and infections and could be promising for TB treatment. Methods This review included studies on the activity of anti-malarial drugs, specifically quinolones and artemisinins, against Mycobacterium tuberculosis complex (MTC), summarizing results from in vitro, in vivo (animal models) studies, and clinical trials. Studies on drugs not primarily developed for TB (doxycycline, sulfonamides) and any novel developed compounds were excluded. Analysis focused on in vitro activity (minimal inhibitory concentrations), synergistic effects, pre-clinical activity, and clinical trials. Results Nineteen studies, including one ongoing Phase 1 clinical trial, were analysed: primarily investigating quinolones like mefloquine and chloroquine, and, to a lesser extent, artemisinins. In vitro findings revealed high MIC values for anti-malarials versus standard TB drugs, suggesting a limited activity. Synergistic effects with anti-TB drugs were modest, with some synergy observed in combinations with isoniazid or pyrazinamide. In vivo animal studies showed limited activity of anti-malarials against MTC, except for one study of the combination of chloroquine with isoniazid. Conclusions The repurposing of anti-malarials for TB treatment is limited by high MIC values, poor synergy, and minimal in vivo effects. Concerns about potential toxicity at effective dosages and the risk of antimicrobial resistance, especially where TB and malaria overlap, further question their repurposing. These findings suggest that focusing on novel compounds might be both more beneficial and rewarding.

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“…Quinoline is a privileged scaffold for bioactive molecules [ 1 , 2 , 3 , 4 , 5 , 6 ]. Shown in Figure 1 are some quinoline-containing drug molecules, including Mefloquine (antimalarial) [ 7 , 8 , 9 , 10 ], Brequinar (anticancer) [ 11 , 12 , 13 ], Pitavastatin (cholesterol-lowering) [ 14 , 15 , 16 ], Plaquenil (antimalarial) [ 17 , 18 ], Ciprofloxacin (antibacterial) [ 19 , 20 , 21 ], and Lenvatinib (anticancer) [ 22 , 23 , 24 ]. Other than these commercial drugs, a great number of quinoline derivatives have been reported or are under development as druggable molecules for anticancer [ 25 , 26 ], antibacterial [ 27 , 28 , 29 ], antifungal [ 30 , 31 , 32 ], antiviral [ 33 , 34 , 35 , 36 ], antimalarial [ 37 , 38 , 39 ], antioxidant [ 40 , 41 , 42 ], anti-inflammatory [ 43 , 44 , 45 ], CNS effect [ 46 , 47 ], cardiovascular, anticonvulsant, analgesic, and anthelmintic rese...…”

Section: Introductionmentioning

confidence: 99%

2-Azidobenzaldehyde-Based [4+2] Annulation for the Synthesis of Quinoline Derivatives

Zhang,

Liu,

Qiu

et al. 2024

Molecules

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Quinoline is a privileged heterocyclic ring which can be found in many drug molecules and bioactive compounds. The development of synthetic methods for making quinoline derivatives continuously attracts the interest of organic and medicinal chemists. This paper highlights 2-azidobenzaldehyde-based [4+2] annulation for the synthesis of quinoline derivatives including fused and spiro-quinolines, quinoline-4-ols, 4-aminoquinolines, and related compounds.

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Mefloquine synergism with anti-tuberculosis drugs and correlation to membrane effects: Biologic, spectroscopic and molecular dynamics simulations studies

Cited by 8 publications

References 67 publications

Design and Management of Control System for Rural Tourism Network Information Based on MVC Model

Design and Management of Control System for Rural Tourism Network Information Based on MVC Model

Repurposing of anti-malarial drugs for the treatment of tuberculosis: realistic strategy or fanciful dead end?

2-Azidobenzaldehyde-Based [4+2] Annulation for the Synthesis of Quinoline Derivatives

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