A new trimeric hispidin derivative, phellinstatin, was isolated from a culture broth of the medicinal fungus Phellinus linteus and its structure was established by various spectral analysis. Phellinstatin strongly inhibited Staphylococcus aureus enoyl-ACP reductase with an IC(50) of 6 μM and also showed antibacterial activity against S. aureus and MRSA.
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http://dx.doi.org/10.1016/j.bmcl.2011.01.080 | DOI Listing |
Colloids Surf B Biointerfaces
April 2025
Laboratory of Applied Toxicology, Center of Toxins, Immune-Response and Cell Signaling - CeT-ICS/CEPID, Butantan Institute São Paulo, São Paulo, SP CEP 05503-900, Brazil; Postgraduate Program Interunits in Biotechnology, USP/IPT/IBU, São Paulo, SP, Brazil. Electronic address:
Background: Irresponsible and wholesale use of antimicrobial agents is the principal cause of the emergence of strains of resistant microorganisms to traditional drugs. Oligoventin is a neutral peptide isolated from spider eggs of Phoneutria nigriventer, with antimicrobial activity against Gram-positive, Gram-negative, and yeast organisms. However, the molecular target and pathways of antimicrobial activity are still unknown.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Guangxi Key Laboratory of Drug Discovery and Optimization, School of Pharmacy, Guilin Medical University, Guilin, 541199, China. Electronic address:
In this study, a series of novel thieno [3, 2-b]pyridinone derivatives were designed and synthesized using a scaffold hopping strategy. Six compounds showed potent anti-mycobacterial activity (minimum inhibitory concentration (MIC) ≤ 1 μg/mL) against Mycobacterium tuberculosis (Mtb) UAlRa. Compound 6c displayed good activity against Mtb UAlRv (MIC = 0.
View Article and Find Full Text PDFRSC Adv
July 2024
Department of Chemistry, Birla Institute of Technology and Science Pilani, Hyderabad Campus, Jawahar Nagar Hyderabad 500 078 Telangana India +91 40 66303527.
Twenty-eight compounds, , 1,8-naphthyridine-3-carbonitrile (ANC and ANA) derivatives, were designed and synthesized through a molecular hybridization approach. The structures of these compounds were analyzed and confirmed using H NMR, C NMR, LCMS, and elemental analyses. The synthesized compounds were evaluated by testing for their effectiveness against tuberculosis using the MABA assay, targeting the H37Rv strain.
View Article and Find Full Text PDFACS Omega
May 2024
Laboratório de Bioinformática e Química Medicinal, Fundação Oswaldo Cruz, CEP: 76812-245 Porto Velho-RO, Brazil.
Malaria, caused by Plasmodium protozoa with as the most virulent species, continues to pose significant health challenges. Despite the availability of effective antimalarial drugs, the emergence of resistance has heightened the urgency for developing novel therapeutic compounds. In this study, we investigated the enoyl-ACP reductase enzyme of (PfENR) as a promising target for antimalarial drug discovery.
View Article and Find Full Text PDFComput Biol Chem
August 2024
Programa de pós-graduação em Biotecnologia, Universidade Estadual de Feira de Santana, Brazil; Programa de pós-graduação em Ciências Farmacêuticas, Universidade Estadual de Feira de Santana, Brazil; Laboratório de Modelagem Molecular, Universidade Estadual de Feira de Santana, Brazil. Electronic address:
Malaria is one of most widespread infectious disease in world. The antimalarial therapy presents a series of limitations, such as toxicity and the emergence of resistance, which makes the search for new drugs urgent. Thus, it becomes necessary to explore essential and exclusive therapeutic targets of the parasite to achieve selective inhibition.
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