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Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication |
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| Authors: | Skerlj Renato Bridger Gary Zhou Yuanxi Bourque Elyse Langille Jonathan Di Fluri Maria Bogucki David Yang Wen Li Tongshuang Wang Letian Nan Susan Baird Ian Metz Markus Darkes Marilyn Labrecque Jean Lau Gloria Fricker Simon Huskens Dana Schols Dominique |
| Institution: | a Genzyme Corp., 153 Second Avenue, Waltham, MA 02451, USA b AnorMED, Inc., 200-20353 64th Avenue, Langley, British Columbia, Canada V2Y 1N5 c Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium |
| Abstract: | A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. |
| Keywords: | CCR5 Chemokine receptor HIV-1 Schering C |
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