New Synthesis and Biological Evaluation of Benzothiazole Derivates as Antifungal Agents

In search of new antifungal agrochemicals that could replace commercially available, aryl-2-mercaptobenzothiazoles were synthesized. They were prepared by two methodologies, using both photostimulated reaction and microwave assisted reaction. These reactions took place without the use of metallic ca...

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Veröffentlicht in:Journal of agricultural and food chemistry 2015-04, Vol.63 (14), p.3681-3686
Hauptverfasser: Herrera Cano, Natividad, Ballari, María S, López, Abel G, Santiago, Ana N
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Sprache:eng
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Zusammenfassung:In search of new antifungal agrochemicals that could replace commercially available, aryl-2-mercaptobenzothiazoles were synthesized. They were prepared by two methodologies, using both photostimulated reaction and microwave assisted reaction. These reactions took place without the use of metallic catalyst by a one-pot procedure with excellent yields (70–98%). Synthesized compounds were evaluated for fungal growth inhibition against Botrytis cinerea. Most of the compounds have an excellent antifungal activity, and three of these showed a superior inhibitory effect to commercial fungicide Triadimefon. IC50 values observed for 2-(phenylthio)­benzothiazole, 2-(2-chlorophenylthio)­benzothiazole, and 2-(3-chlorophenyl thio)­benzothiazole were 0.75, 0.69, and 0.65 μg mL–1, respectively.
ISSN:0021-8561
1520-5118
DOI:10.1021/acs.jafc.5b00150