Synthesis of Allylthiopyridazine Derivatives and Inhibition of Aflatoxin B1-Induced Hepatotoxicity in Rats

Shin, Hea-Soon; Kwon, Soon-Kyoung

doi:10.1007/bf02976691

Cited by 9 publications

(1 citation statement)

References 20 publications

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“…Combination of the latex of Euphorbia characias , known to contain a high concentration of terpenes, with ketoconazole also resulted in synergistic antifungal activity against C. albicans in in vitro assays (Giordani et al, 2001). The essential oil of Pelargonium graveolens , used in the perfume industry, and its main components, geraniol and citronellol, had additive and synergistic in vitro antifungal activity against two species of Aspergillus , in combination with AMB or ketoconazole (Shin, 2003). Another in vitro examination of the essential oil of P. graveolens in combination with nystatin showed some synergistic activity against clinical strains and species of Candida , but not to the extent of the synergistic interaction of nystatin with the essential oil from Origanum vulgare (oregano; Rosato et al, 2009).…”

Section: Chemosensitization Of Antifungal Agentsmentioning

confidence: 99%

Chemosensitization as a Means to Augment Commercial Antifungal Agents

2012

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Antimycotic chemosensitization and its mode of action are of growing interest. Currently, use of antifungal agents in agriculture and medicine has a number of obstacles. Foremost of these is development of resistance or cross-resistance to one or more antifungal agents. The generally high expense and negative impact, or side effects, associated with antifungal agents are two further issues of concern. Collectively, these problems are exacerbated by efforts to control resistant strains, which can evolve into a treadmill of higher dosages for longer periods. This cycle in turn, inflates cost of treatment, dramatically. A further problem is stagnation in development of new and effective antifungal agents, especially for treatment of human mycoses. Efforts to overcome some of these issues have involved using combinations of available antimycotics (e.g., combination therapy for invasive mycoses). However, this approach has had inconsistent success and is often associated with a marked increase in negative side effects. Chemosensitization by natural compounds to increase effectiveness of commercial antimycotics is a somewhat new approach to dealing with the aforementioned problems. The potential for safe natural products to improve antifungal activity has been observed for over three decades. Chemosensitizing agents possess antifungal activity, but at insufficient levels to serve as antimycotics, alone. Their main function is to disrupt fungal stress response, destabilize the structural integrity of cellular and vacuolar membranes or stimulate production of reactive oxygen species, augmenting oxidative stress and apoptosis. Use of safe chemosensitizing agents has potential benefit to both agriculture and medicine. When co-applied with a commercial antifungal agent, an additive or synergistic interaction may occur, augmenting antifungal efficacy. This augmentation, in turn, lowers effective dosages, costs, negative side effects and, in some cases, countermands resistance.

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Section: Chemosensitization Of Antifungal Agentsmentioning

confidence: 99%

Chemosensitization as a Means to Augment Commercial Antifungal Agents

2012

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Design, Synthesis, and Biological Evaluation of Selenium‐incorporated Aminopyridazines as Anticancer Agents

Kim

Jung

et al. 2015

Bulletin Korean Chem Soc

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A new series of 3-alkylseleno-6-alkylaminopyridazines, 3-alkylseleno-6-alkyliminopyridazines, and 3-alkylseleno-6-dialkylaminopyridazines was synthesized from 3,6-dichloropyridazine for development of new anticancer agents. The process involves the selenylation, Se-alkylation, and aralkylamination (or imination). The alkylamines such as ethylamine and the dialkylamines such as dipropylamine were introduced into the 3-position of the pyridazine ring. These new compounds showed antiproliferative activities against breast cancer (MCF-7) and hepatocellular carcinoma (Hep3B) cells in CCK-8 assays and could be promising candidates for chemotherapy of carcinomas.

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Synthesis of 3-alkylthio-6-allylthiopyridazine derivatives and their antihepatocarcinoma activity

Kwon

Moon

2005

Arch Pharm Res

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The allylthio group of allicin and other organosulfur compounds, isolated from garlic, is considered a pharmacophore, and a key structure component of the molecule, which affords biological activities. In the foregoing studies, various 3-alkoxy-6-allylthiopyridazine derivatives (K-compounds) were synthesized, and their biological activities tested in animals. As expected, the various derivatives showed good hepatoprotective activities on carbon tetrachloride-treated mice and aflatoxin B1-treated rats, and chemopreventive activities on hepatocarcinoma cells in rats. Other new pyridazine derivatives, with the oxygen atom at the 3-position of the 3-alkoxy-6-allylthiopyridazine displaced by sulfur (S), were synthesized, and their activities tested in vitro. Thio-K6, one of the sulfur-substituted compounds, showed better chemopreventive activity toward hepatocarcinoma cells.

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Synthesis of Allylthiopyridazine Derivatives and Inhibition of Aflatoxin B1-Induced Hepatotoxicity in Rats

Cited by 9 publications

References 20 publications

Chemosensitization as a Means to Augment Commercial Antifungal Agents

Chemosensitization as a Means to Augment Commercial Antifungal Agents

Design, Synthesis, and Biological Evaluation of Selenium‐incorporated Aminopyridazines as Anticancer Agents

Synthesis of 3-alkylthio-6-allylthiopyridazine derivatives and their antihepatocarcinoma activity

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