Abstract
Objective: The objective of the study was to evaluate the therapeutic indices (TIs) some antifungal organic compounds and to compare their safety.
 Methods: TIs of 55 organic compounds were evaluated by dividing their mammalian toxicity values given as median lethal doses ([mg/kg] rat, oral) collected from literature by experimentally determined fungitoxicity values evaluated as median effective concentration (EC50 [mg/L]) for the mycelial growth inhibition of Colletotrichum gloeosporioides on potato dextrose agar medium.
 Results: Large variations in TIs are observed in different classes of compounds, namely, alcohols, carboxylic acids, phenols, esters, and aldehydes. The relationship between carbon chain length of saturated monohydric alcohols and mammalian toxicity shows that toxicity increases from chain length 1 to 5, declines from 5 to 6, increases from 6 to 7, and steadily declines from 7 to 10. Thus, the relationship is by and large parabolic. The relationship between carbon chain length and molar antifungal activity is also parabolic. In spite of this, large differences are found in TIs making 1-decanol (TI=42.1) a very safe antifungal compound and 1-pentanol (TI=0.17) a hazardous antifungal compound. This is because mammalian toxicity reaches a maximum around carbon chain length of 5, while in the case of antifungal activity, it reaches a maximum around carbon chain length of 10.
 Conclusions: Among the 55 compounds, whose TIs were evaluated, some compounds with high TIs (>10) which can be considered safe as antifungal compounds are citronellol, geraniol, 1-decanol, 1-octanol, phenyl acetaldehyde, methyl anthranilate, 1-naphthol, 2-naphthol, and propionic acid. Some compounds with low TIs (<0.50) which can be considered hazardous as antifungal compounds are resorcinol, hydroquinone, oxalic acid, and acetyl acetone.
Highlights
Fungi are the causal organisms of many diseases of man, animals, and plants
Among the 55 compounds, whose therapeutic indices (TIs) were evaluated, some compounds with high TIs (>10) which can be considered safe as antifungal compounds are citronellol, geraniol, 1-decanol, 1-octanol, phenyl acetaldehyde, methyl anthranilate, 1-naphthol and 2-naphthol
Some compounds with low TIs (
Summary
Fungi are the causal organisms of many diseases of man, animals, and plants. They cause post-harvest spoilage of agricultural products. Therapeutic index (TI) [10,11] known as selective toxicity coefficient [12,13] which is the ability of a compound to injure one kind of living matter without harming some other kind even though both are in intimate contact is considered as an important criterion for recommending any compound for its safe use as antifungal compound Since this awareness is important, TI values of 55 common organic compounds whose antifungal activity values had been reported earlier from this institute [5,6,7,8,9] were evaluated and are reported in this paper. The variation in the case of monohydric saturated straight chain alcohols is interpreted in terms of SAR studies
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