Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties

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 D...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Hauptverfasser:	POPOV VELJKO, BOLSTAD DAVID B, BOLSTAD ERIN S. D, WRIGHT DENNIS L, PELPHREY PHILLIP M, JOSKA TAMMY M, ANDERSON AMY C
Format:	Patent
Sprache:	eng
Schlagworte:	AGRICULTURE ANIMAL HUSBANDRY BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES CHEMISTRY FISHING FORESTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HUNTING HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEST REPELLANTS OR ATTRACTANTS PLANT GROWTH REGULATORS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF TRAPPING
Online-Zugang:	Volltext bestellen
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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 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.