کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375951 | 981947 | 2009 | 5 صفحه PDF | دانلود رایگان |
Replacement of the cyclic carbamate in our previously disclosed 1-oxa-3,9-diazaspiro[5.5]undecan-2-one template led to the discovery of two novel series of 3,9-diazaspiro[5.5]undecane and undeca-2-one CCR5 antagonists. The synthesis, SAR, and antiviral activities of these two series are described. One compound (32) was found to have attractive combination of antiviral potency, selectivity, and pharmacokinetic profile. The asymmetric synthesis of 32 was also accomplished and both enantiomers were equally potent.
Two novel series of 3,9-diazaspiro[5.5]undecane and undeca-2-one CCR5 antagonists were discovered. The synthesis, SAR, and antiviral activities of these two series are described. Compound 32 was found to have attractive combination of antiviral potency, selectivity, and pharmacokinetic profile.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 1, 1 January 2009, Pages 209–213