Cyclization of benzene-1,4-dicarbaldehyde dioxime 1 with different aromatic aldehydes in inert atmosphere yielded the corresponding new bisdioxazoles 2-11. The structure of 2-11 was elucidated by spectral data. In vitro antiamoebic activity was performed against HM1:IMSS strain of Entamoeba histolytica. The results showed that the compounds 3 (IC(50)=1.22 microM), 4 (IC(50)=1.41 microM), 7 (IC(50)=1.05 microM) and 10 (IC(50)=1.01 microM) exhibited better antiamoebic activity than the standard drug metronidazole (IC(50)=1.80 microM). The compounds 3, 4, 7 and 10 were tested for toxicity by MTT assay on H9c2 cardiac myoblasts and the results showed that the compounds 3, 4, 7 and 10 offered remarkable viability of 96.2%, 83.5%, 82% and 89%, respectively at a concentration of 12.5 microg/ml.
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http://dx.doi.org/10.1016/j.ejmech.2009.06.016 | DOI Listing |
J Nat Prod
January 2025
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), University of Porto, Avenida General Norton de Matos, s/n4450-208Matosinhos, Portugal.
Genome mining has emerged as an important tool for the discovery of natural products and is particularly effective for the swift identification of ribosomally synthesized and post-translationally modified peptides (RiPPs). Among RiPPs, cyanobactins have gained attention due to their diverse structures and bioactive properties. Here, we explored the Microcoleaceae cyanobacterium LEGE 16532 strain and identified the biosynthetic gene cluster (BGC), which was predicted to encode cyanobactin-like molecules.
View Article and Find Full Text PDFBasic Clin Pharmacol Toxicol
January 2025
Department of Pharmacy, Faculty of Pharmacy, Universitas Borneo Lestari, Banjarbaru, Indonesia.
Adv Synth Catal
December 2023
Department of Chemistry, University of Wisconsin-Madison, Madison, Wisconsin, 53706, United States.
A three-step synthesis of anti-amoebic, ring-fused mackinazolinones has been developed. A Mannich-type reaction between quinazolin-4-ones and -Cbz propanal in the presence of AgOTf afforded quinazolinones (19-94% isolated yield) bearing a newly formed heterocycle with an alkylamine appendage that, upon -Cbz deprotection and basification, triggered a domino rearrangement to afford 45 separable, ring-fused products. Several compounds inhibited growth of parasites that can cause a lethal human brain infection.
View Article and Find Full Text PDFInt J Mol Sci
October 2024
Departamento de Infectómica y Patogénesis Molecular, CINVESTAV-IPN, Ciudad de México 07360, CP, Mexico.
Several studies with kaempferol (KP) and linearolactone (LL) have demonstrated their antiparasitic activity. However, the toxicity of these treatments is unknown. Therefore, this study aimed to evaluate the possible toxicological effects of intraperitoneal (i.
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