6533b835fe1ef96bd129ed40
RESEARCH PRODUCT
Discovery of 2-aryl and 2-pyridinylbenzothiazoles endowed with antimicrobial and aryl hydrocarbon receptor agonistic activities
Rosa M. GinerLaureano E. CarpioFatma AbdmoulehElizabeth Goya-jorgeMaité Sylla-iyarreta Veitíasubject
Staphylococcus aureus[SDV]Life Sciences [q-bio]Pharmaceutical Science02 engineering and technology[CHIM.THER]Chemical Sciences/Medicinal ChemistryAntifungal030226 pharmacology & pharmacyArticleAgonism03 medical and health scienceschemistry.chemical_compound0302 clinical medicineAnti-Infective AgentsEscherichia coli[SDV.BBM]Life Sciences [q-bio]/Biochemistry Molecular BiologyReporter genebiologyArylBenzothiazole021001 nanoscience & nanotechnologyAntimicrobialDruglikenessAryl hydrocarbon receptor[SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/BacteriologyCorpus albicansAntibiofilmAnti-Bacterial Agents3. Good healthAntibacterial[SDV.MP]Life Sciences [q-bio]/Microbiology and ParasitologyReceptors Aryl HydrocarbonBenzothiazolechemistryBiochemistryAh receptorbiology.protein[INFO.INFO-BI]Computer Science [cs]/Bioinformatics [q-bio.QM]0210 nano-technologyEndogenous agonistdescription
Highlights • Sixteen functionalized benzothiazoles were evaluated as antimicrobial agents and as AhR modulators. • The benzothiazoles showed noticeable antimicrobial effects against Gram-positive and Gram-negative pathogens and against the yeast C. albicans. • Six benzothiazoles exhibited significant AhR agonist effects in a cell-based reporter gene assay. • Structure-activity relationship analysis exposed some relevant headings on the substituent's contributions to the studied biological effects. • Compound 12 displayed promising biocide activity and AhR agonism as well as an adequate ADMET profile and binding similarities with FICZ.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2020-05-01 |