Inventors:
Amy C. Anderson - Storrs CT, US
Dennis L. Wright - Storrs CT, US
Phillip M. Pelphrey - Williamsville NY, US
Tammy M. Joska - Hartford VT, US
Erin S.D. Bolstad - Vernon CT, US
David B. Bolstad - Vernon CT, US
Veljko Popov - Hanover NH, US
Assignee:
University of Connecticut - Farmington CT
International Classification:
A61K 31/505, C07D 239/42, A61P 31/04, A61P 31/10, A61P 33/02
Abstract:
The compositions and methods described herein discloses 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 and methicillin-resistant , fungi such as and and protozoa such as and . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.