ChemInform Abstract: Discovery of 1,6-Naphthyridines as a Novel Class of Potent and Selective Human Cytomegalovirus Inhibitors.

✍ Scribed by Laval Chan; Haolun Jin; Tomislav Stefanac; Jean-Francois Lavallee; Guy Falardeau; Wei Wang; Jean Bedard; Suzanne May; Leonard Yuen

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 32 KB
• Volume: 30
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199952157

✦ Synopsis

Discovery of 1,6-Naphthyridines as a Novel Class of Potent and Selective Human Cytomegalovirus Inhibitors.

-A series of 20 1,6-naphthyridines, e.g. (I), is synthesized by amidation of key intermediate (IV) and in case of its halogen analogue (V) by subsequent Stille coupling with stannanes, e.g. (VII). Among them, compounds (If), (Ig), and (Ih) exhibit high potency and excellent selectivity as human cytomegalovirus inhibitors. Further studies of this class of compounds concerning structure-activity relationship, mechanisms, and pharmacokinetics are under way.

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