933697-03-1Relevant academic research and scientific papers
Discovery, synthesis, and biological evaluation of a novel group of selective inhibitors of filoviral entry
Yermolina, Maria V.,Wang, Jizhen,Caffrey, Michael,Rong, Lijun L.,Wardrop, Duncan J.
experimental part, p. 765 - 781 (2011/04/15)
Herein, we report the development of an antifiloviral screening system, based on a pseudotyping strategy, and its application in the discovery of a novel group of small molecules that selectively inhibit the Ebola and Marburg glycoprotein (GP)-mediated infection of human cells. Using Ebola Zaire GP-pseudotyped HIV particles bearing a luciferase reporter gene and 293T cells, a library of 237 small molecules was screened for inhibition of GP-mediated viral entry. From this assay, lead compound 8a was identified as a selective inhibitor of filoviral entry with an IC50 of 30 μM. To analyze functional group requirements for efficacy, a structure-activity relationship analysis of this 3,5-disubstituted isoxazole was then conducted with 56 isoxazole and triazole derivatives prepared using "click" chemistry. This study revealed that while the isoxazole ring can be replaced by a triazole system, the 5-(diethylamino)acetamido substituent found in 8a is required for inhibition of viral-cell entry. Variation of the 3-aryl substituent provided a number of more potent antiviral agents with IC50 values ranging to 2.5 μM. Lead compound 8a and three of its derivatives were also found to block the Marburg glycoprotein (GP)-mediated infection of human cells.
Identification of phenylisoxazolines as novel and viable antibacterial agents active against gram-positive pathogens
Barbachyn, Michael R.,Cleek, Gary J.,Dolak, Lester A.,Garmon, Stuart A.,Morris, Joel,Seest, Eric P.,Thomas, Richard C.,Toops, Dana S.,Watt, William,Wishka, Donn G.,Ford, Charles W.,Zurenko, Gary E.,Hamel, Judith C.,Schaadt, Ronda D.,Stapert, Douglas,Yagi, Betty H.,Adams, Wade J.,Friis, Janice M.,Slatter, J. Gregory,Sams, James P.,Oien, Nancee L.,Zaya, Matthew J.,Wienkers, Larry C.,Wynalda, Michael A.
, p. 284 - 302 (2007/10/03)
A new and promising group of antibacterial agents, collectively known as the oxazolidinones and exemplified by linezolid (PNU-100766, marketed as Zyvox), have recently emerged as important new therapeutic agents for the treatment of infections caused by G
Fungicidal 3-phenyl-5-(substituted methyl) isoxaxoles
-
, (2008/06/13)
A class of isoxazoles having a phenyl or substituted-phenyl group at the 3-position and a substituted-methyl group at the 5-position are useful for the control of fungal foliar phytopathogens.
