Novel series of long chain isoxazole derivatives were designed as inhibitors of Cytochrome P450-14DM14a-demethylase from Candida albicans and ribosomal subunit of S12 protein from Escherichia coli. The novel compounds (6-10) were synthesized through 1,3-dipolar cycloaddition of nitrile oxide to long chain alkynoic acid and alkenyl/hydroxyalkenyl esters and tested for their antimicrobial activity by disk diffusion assay and MIC by broth micro dilution method. After predicting the hidden potential and drug-likeness of compounds, ADMET-related descriptors were also calculated to predict pharmacokinetic properties. Molecular docking studies have been performed to evaluate possible mode of action of molecules in active site of receptor. Compounds (9 and 10) showed excellent antimicrobial activity nearly equivalent to the control compounds.
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http://dx.doi.org/10.1016/j.ejmech.2013.10.051 | DOI Listing |
Biochem Genet
January 2025
Key Laboratory of Parasite and Vector Biology of the Chinese Ministry of Health, Chinese Center for Disease Control and Prevention, WHO Collaborating Centre for Tropical Diseases, National Institute of Parasitic Diseases, Shanghai, 200025, People's Republic of China.
Drug resistance resulting from mutations in Plasmodium falciparum, that caused the failure of previously effective malaria drugs, has continued to threaten the global malaria elimination goal. This study describes the profiles of P. falciparum chloroquine resistance transporter (Pfcrt) and P.
View Article and Find Full Text PDFMol Biol Rep
January 2025
Laboratory of Genomics and Human Genetics, Institut Pasteur du Maroc, Casablanca, Morocco.
Background: Male infertility (MI) is a polygenic condition mainly induced by spermatogenic failure/arrest or systemic disease with a large clinical spectrum. Lately, genetic sequencing allowed the identification of several variants implicated in both aforesaid situations.
Methods And Results: In this case study, we performed whole exome sequencing (WES) on the genomic DNA of a 37-year-old Moroccan man with Non-Obstructive Azoospermia.
J Fish Biol
January 2025
Marine Biology, Ghent University, Ghent, Belgium.
The European eel (Anguilla anguilla L.) exhibits a remarkable phenotypic plasticity by occupying both marine and freshwater habitats and transitional areas in between. Because these habitats are characterized by different food sources with different fatty acid compositions, it remains unclear how eels from different habitats obtain essential long-chain polyunsaturated fatty acids (LC-PUFAs) to integrate in their lipids.
View Article and Find Full Text PDFTurk J Gastroenterol
January 2025
Department of Gastrointestinal Surgery, Provincial Hospital Affiliated to Shandong First Medical University, Jinan, China.
Background/aims: Cholangiocarcinoma (CCA) is a malignant and insidious tumor that is tricky to treat. Long non-coding RNA (LncRNA) LINC01123 is a biomolecule that influences cancer progression by regulating gene expression via influencing the regulatory function of microRNAs in gene expression. Therefore, this study investigated the connection between LINC01123 and CCA and explored the underlying mechanism.
View Article and Find Full Text PDFAdv Mater
January 2025
Faculty of Materials Science and Engineering, South China University of Technology, Guangzhou, 510640, P. R. China.
Dynamic covalent polymer networks (DCPN) provide an important solution to the challenging recyclability of thermoset elastomers. However, dynamic bonds exhibit relatively weak bond energies, considerably decreasing the mechanical properties of DCPN. Herein, a novel reinforcement strategy for DCPN involving the in situ formation of supramolecular organic nanofillers through asynchronous polymerization is proposed.
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