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Antifungal properties of a novel 1,2,4-triazine derivative I 319
Abstract:
The antifungal activity of the sodium salts, of 3-thiolo-5-phenyl-1,2,4-triazine (I 319) was determined in vitro and in vivo. The minimal inhibitory concentration (MIC) of I 319 for 33 pathogenic and saprophytic fungal strains ranged from 3.1 to 25 microgram/ml. In vivo, experiments were performed on a model of subacute candidiasis in Balb/c mice infected intraperitoneally with Candida albicans. The antifungal activity was estimated on the basis of the extension of the mice life span and on the number of living yeast cells present in the kidneys, liver and spleen of treated and control mice. A single i.p. dose of I 319 (25 mg/kg) prolonged the survival time of treated animals up to 200%. Five subsequent doses of the compound diminished the number of C. albicans cells in the tissues of these mice. The DL50 of I 319 for mice (i.p.) was about 250 mg/kg.
Insights
The sodium salt of 3-thiolo-5-phenyl-1,2,4-triazine (I 319) shows potent antifungal activity against pathogenic fungi. In vivo studies demonstrated significant survival benefits in a mouse model of candidiasis.
Area of Science:
- Mycology
- Pharmacology
- Infectious Diseases
Background:
- Fungal infections pose a significant global health challenge, necessitating the development of novel antifungal agents.
- Candida albicans is a common opportunistic pathogen responsible for various infections, from superficial to life-threatening systemic candidiasis.
- The development of effective antifungal therapies with favorable safety profiles remains a critical area of research.
Purpose of the Study:
- To evaluate the in vitro and in vivo antifungal efficacy of the sodium salt of 3-thiolo-5-phenyl-1,2,4-triazine (I 319).
- To determine the minimal inhibitory concentration (MIC) of I 319 against a range of fungal strains.
- To assess the therapeutic potential of I 319 in a murine model of subacute candidiasis.
Main Methods:
- In vitro antifungal activity was assessed by determining the minimal inhibitory concentration (MIC) against 33 fungal strains.
- In vivo efficacy was evaluated using a subacute candidiasis model in Balb/c mice infected with Candida albicans.
- Antifungal activity in vivo was measured by changes in animal lifespan and quantification of fungal burden in key organs (kidneys, liver, spleen).
Main Results:
- The minimal inhibitory concentration (MIC) of I 319 ranged from 3.1 to 25 microgram/ml against 33 pathogenic and saprophytic fungal strains.
- A single intraperitoneal (i.p.) dose of I 319 (25 mg/kg) increased the survival time of infected mice by up to 200%.
- Multiple doses of I 319 significantly reduced the number of Candida albicans cells in the kidneys, liver, and spleen of treated mice.
Conclusions:
- The sodium salt of 3-thiolo-5-phenyl-1,2,4-triazine (I 319) exhibits significant in vitro and in vivo antifungal activity.
- I 319 demonstrates therapeutic potential for treating Candida albicans infections, as evidenced by increased survival and reduced fungal burden in a murine model.
- Further investigation into I 319 as a potential antifungal drug candidate is warranted.