期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 18, 页码 5880-5884出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm800792b
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资金
- NIH [GM41916]
- New Zealand Foundation for Research, Science Technology
The potent immucillin purine nucleoside phosphorylase (PNP) inhibitors F-DADMe-ImmH [(3S,4S)-3], and [(3R,4R)-3] are synthesized in seven steps. Cycloaddition to a fluoroalkene and an enzymic resolution are the key features of the construction of the fluoropyrrolidines 11, from which the immucillins are assembled by use of a three-component Mannich reaction. Slow-onset binding constants (K(i)*) for [(3S,4S)-3] and [(3R,4R)-3] with human PNP are 0.032 and 1.82 nM, respectively. F-DADMe-ImmH [(3S,4S)-3] exhibits oral availability in mice at doses as low as 0.2 mg/kg.
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