Background COVID-19 is an ongoing viral pandemic produced by SARS-CoV-2. In light of in vitro efficacy, several medications were repurposed for its management. During clinical use, many of these medications produced inconsistent results or had varying limitations. Objective The purpose of this literature review is to explain the variable efficacy or limitations of Lopinavir/Ritonavir, Remdesivir, Hydroxychloroquine, and Favipiravir in clinical settings. Method A study of the literature on the pharmacodynamics (PD), pharmacokinetics (PK), safety profile, and clinical trials through academic databases using relevant search terms. Results & Discussion The efficacy of an antiviral drug against COVID-19 is associated with its ability to achieve therapeutic concentration in the lung and intestinal tissues. This efficacy depends on the PK properties, particularly protein binding, volume of distribution, and half-life. The PK and PD of the model drugs need to be integrated to predict their limitations. Conclusion Current antiviral drugs have varying pharmacological constraints that may associate with limited efficacy, especially in severe COVID-19 patients, or safety concerns. Disclaimer What was mentioned in this paper is a scientific view and information relating to general principles which should not be construed as specific instructions to change or criticize any protocols. But rather an academic discussion to push further research and development of these drugs for better achievements.
Background While the frequency of methicillin-resistant Staphylococcus aureus (MRSA) continues to rise globally, there is a fear regarding an increase in vancomycin resistance among S. aureus strains. As far back as the 1960s, MRSA was one of the world’s most prevalent antibiotic-resistant bacteria. Among hospitalized patients and community members, MRSA is the cause of a significant number of infections. As a result of its resistance to classical beta-lactam and, in some cases, vancomycin antibiotics, efforts must be made as soon as feasible to find a new approach to fighting MRSA. Purpose This study is designed to evaluate the antibacterial activity of quinoxaline derivative compound against MRSA in comparison with vancomycin as a reference drug. Methods Sixty MRSA isolates were subjected to susceptibility testing by broth microdilution method for quinoxaline derivative compound and vancomycin. Each drug’s minimal inhibitory concentration (MIC) was determined and compared. Results Among the sixty MRSA isolates, most of the quinoxaline derivative compound MIC findings (56.7%) were 4 µg/mL compared to vancomycin MIC values (63.3%) of 4 µg/mL. In comparison, 20% of quinoxaline derivative compound MIC readings were 2 µg/mL, while the vancomycin MIC results were 6.7%. However, the overall proportion of MIC readings at ≤2 µg/mL for both antibacterial agents was equal (23.3%). None of the isolates were resistant to vancomycin. Conclusion This experiment revealed that most MRSA isolates were associated with low MICs (1–4 μg/mL) for quinoxaline derivative compound. Overall, the susceptibility of the quinoxaline derivative compound signifies a promising efficacy against MRSA and may set a novel treatment approach.
Background: 2,3-dimethylquinoxaline (DMQ) is a naturally occurring compound with documented antifungal activity. It showed also good in vitro physicochemical and pharmacokinetic characteristics. Methods: The wound healing activity of 1% DMQ hydrogel in healthy adult male Wister rats were evaluated using the excision wound model. On day 7, the mean percentage closure of the wound area was determined. The animals were sacrificed on day 7 and skin was isolated for histology research and assessment of some inflammatory & oxidative markers, hydroxyproline and tissue growth factor. Results and Discussion: Almost complete wound healing was observed after treatment with DMQ 1 % Jell for 7 days. The histological study confirmed marked attenuation of wound-induced histological changes. There was a marked reduction in TNF-α, IL-6 IL-β1 and NF-κB. levels. These data suggest the potential anti-inflammatory effect of DMQ. Conclusion: DMQ has potential skin wound healing ability likely due to its anti-inflammatory mechanism. Further study is needed to confirm these preliminary findings and explore the molecular mechanism
Aims: To explore the antifungal activity of 2,3-dimethylquinoxaline. Study Design: A preclinical study of a compound against 10 fungal species. Backgrounds: Severe fungal infections cause significant clinical problem and need more effort to search for new antifungals. Methodology: We evaluated the susceptibility of 2,3-dimethylquinoxaline in vitro against a wide range of pathogenic fungi, including six Candida species, two Aspergillus species, one Cryptococcus species, and one Trichophyton species. Also, we evaluated the susceptibility of 2,3-dimethylquinoxaline in vivo against oral candidiasis using a mice model. Results: The highest score of the minimum inhibitory concentration was 9 µg/ml against Cryptococcus neoformans. While, the lowest score was 1125 µg/ml against Candida tropicalis. The oral candidiasis in a mouse model was resolved using 2,3-dimethylquinoxaline 1% gel. Conclusion: The 2,3-Dimethyquinoxaline has interesting antifungal activity. Quinoxalines in general need to be further developed as a promising antifungal candidate.
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