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Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity.

Andrew Matheus Frederico RozadaFrancielli Abigail Vilugron RodriguesÉrika Seki KioshimaEloísa Gibin SampironRegiane Bertin de Lima ScodroKatiany Rizzieri Caleffi FerracioliFlavio Augusto Vicente SeixasErnani Abicht BassoGisele de Freitas Gauze
Published in: Future medicinal chemistry (2023)
Background: Paracoccidioidomycosis (PCM) is a systemic infection caused by Paracoccidioides spp. ( Pb ). PCM can be associated or clinically confused with tuberculosis (TB), another pulmonary infection, caused by Mycobacterium tuberculosis ( Mtb ). Futhermore, the long treatment time of TB and PCM and the cases of TB drug resistance impose difficulties for the cure of these diseases. Results: New 1,3,4-oxadiazoles containing the 4-methoxynaphthalene ring were synthesized and their antimicrobial activity was evaluated against Pb and Mtb . The derivative 6n (with 2-hydroxy-5-nitrophenyl subunit) is the most promising of the series. Conclusion: The 1,3,4-oxadiazole 6n can be used as a prototype drug candidate, with anti- Pb and anti- MTb activities, showing a broad-spectrum profile for the treatment of both pulmonary infections.
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