Article
Carbamoyl pyridone HIV-1 integrase inhibitors. 1. Molecular design and establishment of an advanced two-metal binding pharmacophore.
Journal of medicinal chemistry - 25 Oct 2012
Kawasuji Takashi, Johns Brian A, Yoshida Hiroshi, Taishi Teruhiko, Taoda Yoshiyuki, Murai Hitoshi, Kiyama Ryuichi, Fuji Masahiro, Yoshinaga Tomokazu, Seki Takahiro, Kobayashi Masanori, Sato Akihiko, Fujiwara Tamio
Abstract excerpt
Our group has focused on expanding the scope of a two-metal binding pharmacophore concept to explore HIV-1 integrase inhibitors through medicinal chemistry efforts to design novel scaffolds which allow for improvement of pharmacokinetic (PK) and resistance profiles. A novel chelating scaffold was rationally designed to effectively coordinate two magnesium cofactors and to extend an aromatic group into an optimal...
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