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The Antimicrobial Activity, Toxicity and Antimicrobial Mechanism of a New Type of Tris(alkylphenyl)sulfonium

机译:新型三(烷基苯基)s的抗菌活性,毒性和抗菌机理

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??The antimicrobial activity, toxicity and antimicrobial mechanism of a new type of tris(4-alkylphenyl)sulfonium which has sterically bulky alkyl substituents (bTAPS), were estimated and compared with those of other sulfoniums which we reported previously. Concerning tris {4-(iso -propyl)phenyl}sulfonium (bTAPS-iso3) and tris{4-(tert -butyl)phenyl}sulfonium (bTAPS-tert4), the antimicrobial activity of these compounds tended to be lower than both tri(n -alkyl)sulfoniums (TASs) and tris{4-(n -alkylphenyl)}sulfoniums (TAPSs) at similar ClogP values. However, the activities of tris{4-(cyclohexyl)phenyl}sulfonium (bTAPS-cyclo6) were clearly higher than those of TAS and were almost similar to those of TAPS at similar ClogP values. The mutagenicities of tested bTAPSs were judged to be all negative. Both the acute oral toxicity strength and the acute skin irritation/corrosion toxicity strength tended to follow the order of TAPSs > bTAPSs > TASs. However, only the acute skin irritation/corrosion toxicity strength of bTAPS-cyclo6 was almost as low as that of TAS which has a similar ClogP value to bTAPS-cyclo6. Because bTAPS-cyclo6 has both high antimicrobial activity and low toxicity, this compound might become to be an alternative antimicrobial compound to relatively hazardous antimicrobials which have been widely used in many fields.
机译:估计了具有立体庞大的烷基取代基(bTAPS)的新型三(4-烷基苯基)s的抗菌活性,毒性和抗菌机理,并与我们先前报道的其他sulf进行了比较。关于三{4-(异丙基)苯基} ulf(bTAPS-iso3)和三{4-(叔丁基)苯基}}(bTAPS-tert4),这些化合物具有抗菌活性。在相似的ClogP值下,其均低于三(I-烷基)ulf(TAS)和三{4-(I-烷基苯基)} ulf(TAPS)。但是,三{4-(环己基)苯基} ulf(bTAPS-cyclo6)的活性明显高于TAS,并且在相似的ClogP值下几乎与TAPS相似。被测bTAPSs的致突变性均被判定为阴性。急性口服毒性强度和急性皮肤刺激/腐蚀毒性强度均趋向于TAPS> bTAPS> TAS。但是,只有bTAPS-cyclo6的急性皮肤刺激/腐蚀毒性强度几乎与TAS一样低,而TAS的ClogP值与bTAPS-cyclo6相似。由于bTAPS-cyclo6具有高抗菌活性和低毒性,因此该化合物可能成为已在许多领域广泛使用的相对危险的抗菌药物的替代抗菌化合物。

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