Journal of Medicinal Chemistry · 1994 · 29 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryEnzymologyEnzyme InhibitionLead Compound DesignNucleobase ChemistryPotency OptimizationStructure-activity Relationship AnalysisNucleobase AnaloguesNucleoside AnalogsPhosphorylase ActivationPurine AnalogsPurine AnaloguesPurine ChemistryPyrimidine Analogs
The synthesis and evaluation as inhibitors of purine nucleoside phosphorylase of six 9-deazahypoxanthines (2a-f) are reported. In contrast to reports in the literature of other hypoxanthine-guanine analog pairs, these inhibitors (2a-f) are equipotent with the corresponding 9-deazaguanines.