title: New synthesis and biological evaluation of benzothiazole derivates as antifungal agents.
abstract: 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.
authors: †INFIQC, Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Córdoba, 5000 Argentina.
authors: Natividad
authors: N
authors: Herrera Cano
authors: †INFIQC, Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Córdoba, 5000 Argentina.
authors: María S
authors: MS
authors: Ballari
authors: ‡ICTA, Facultad de Ciencias Exactas, Físicas y Naturales, Universidad Nacional de Córdoba, Ciudad Universitaria, Córdoba, 5000 Argentina.
authors: Abel G
authors: AG
authors: López
authors: †INFIQC, Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Córdoba, 5000 Argentina.
authors: Ana N
authors: AN
authors: Santiago
mesh_terms: D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D020171:Botrytis / Q000187:drug effects; D005659:Fungicides, Industrial / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure
chemical_list: D052160:Benzothiazoles; D005659:Fungicides, Industrial; C005465:benzothiazole
keywords: Botrytis cinerea; antifungal activities; microwave irradiation; synthesis