RESUMO
Twenty-one novel pyrazole-thiazole carboxamide derivatives were rationally designed and synthesized. Bioassay results indicated that 6d (EC50 = 5.11 µg/mL) and 6j (EC50 = 8.14 µg/mL) exhibited better in vitro activities than fluxapyroxad (EC50 = 11.93 µg/mL) and thifluzamide (EC50 = 22.12 µg/mL) against Rhizoctonia cerealis. Particularly, compound 6j showed promising in vivo protective activity against Rhizoctonia solani and Puccinia sorghi Schw. with 80% and 90% inhibition at 10 µg/mL, respectively. Our studies found that pyrazole-thiazole is a promising fungicide lead deserving for further derivation.
Assuntos
Fungicidas Industriais , Antifúngicos/farmacologia , Fungicidas Industriais/farmacologia , Pirazóis/farmacologia , Relação Estrutura-Atividade , Tiazóis/farmacologiaRESUMO
Kidney injuries may trigger renal fibrosis and lead to chronic kidney disease (CKD), but effective therapeutic strategies are still limited. Quercetin is a natural flavonoid widely distributed in herbal medicines. A large number of studies have demonstrated that quercetin may protect kidneys by alleviating renal toxicity, apoptosis, fibrosis and inflammation in a variety of kidney diseases. Therefore, quercetin could be one of the promising drugs in the treatment of renal disorders. In the present study, we review the latest progress and highlight the beneficial role of quercetin in kidney diseases and its underlying mechanisms. The pharmacokinetics and bioavailability of quercetin and its proportion in herbal medicine will also be discussed.