AI Article Synopsis
Article Abstract
A small series of C-glycosides containing the methoxyaryl moieties was tested for the inhibition of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from Cryptococcus neoformans and Brucella suis. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes. The deprotected glycosides incorporating the 6-methoxy-2-naphthyl moiety showed the best inhibition profile and therefore represent leads for the development of novel anti-infectives with a new mechanism of action.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.3109/14756366.2014.967233 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Redox-Active Magnetic Composites for Anionic Contaminant Removal from Water.
ACS Appl Mater Interfaces
February 2022
Department of Chemical Engineering, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.
Global water security is jeopardized by the presence of anthropogenic contaminants, which can persist resiliently in the environment and adversely affect human health. Surface adsorption of polluting species is an effective technique for water purification. In this work, redox-active magnetic compounds were designed for the targeted removal of inorganic and organic anions in water via polymeric redox-active vinylferrocene (VFc) and pyrrole (Py) moieties.
View Article and Find Full Text PDFUse of selective PGE2 receptor antagonists on human endometriotic stromal cells and peritoneal macrophages.
Mol Hum Reprod
January 2021
Department of Obstetrics and Gynecology, The University of Tokyo, Tokyo 113-8655, Japan.
Non-hormonal therapeutic strategies for endometriosis are needed. The aim of this study was to characterize the effects of prostaglandin (PG)E2 receptor inhibitors to explore their potential as novel therapeutic strategies for endometriosis. The expression of PGE2 receptors (EP2 and EP4) in donated tissues from human ovarian endometriosis, adenomyosis and peritoneal endometriosis was examined using immunohistochemistry.
View Article and Find Full Text PDFC-glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases.
J Enzyme Inhib Med Chem
May 2016
a LADECOR, Departamento de Química , Facultad de Ciencias Exactas, Universidad Nacional de La Plata , La Plata , Argentina .
A small series of C-glycosides containing the methoxyaryl moieties was tested for the inhibition of the β-class carbonic anhydrases (CAs, EC 4.2.1.
View Article and Find Full Text PDFExploration of alternate catalytic mechanisms and optimization strategies for retroaldolase design.
J Mol Biol
January 2014
Department of Biochemistry, University of Washington, Seattle, WA 98195, USA; Howard Hughes Medical Institute, University of Washington, Seattle, WA 98195, USA. Electronic address:
Designed retroaldolases have utilized a nucleophilic lysine to promote carbon-carbon bond cleavage of β-hydroxy-ketones via a covalent Schiff base intermediate. Previous computational designs have incorporated a water molecule to facilitate formation and breakdown of the carbinolamine intermediate to give the Schiff base and to function as a general acid/base. Here we investigate an alternative active-site design in which the catalytic water molecule was replaced by the side chain of a glutamic acid.
View Article and Find Full Text PDFInhibition of endonuclease by d-2-(6'-methoxy-2'-naphthyl)-propionic acid (naproxen) is discussed as a possible therapeutic principle of the antiinflammatory action in polyarthritis. Infections by 'slow viruses" and mycoplasma have to be considered as possible etiologic factors for rheumatoid arthritis. The incorporation of the viral or mycoplasmatic DNA into the genetic material of the host cell depends on the function of endonucleases, which can be inhibited by naproxen.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!