Kishore Viswanathan;Kathleen Mary Frey;Dennis L. Wright;Janet Leigh Paulsen;Eric William Scocchera;Amy C. Anderson
发明人:
Amy C. Anderson,Dennis L. Wright,Kathleen Mary Frey,Janet Leigh Paulsen,Eric William Scocchera,Kishore Viswanathan
申请号：
US13290741
公开号：
US20120196859A1
申请日:
2011.11.07
申请国别(地区):
US
年份:
2012
代理人:
摘要：
The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
