- Structure-activity relationship of thiopyrimidines as mGluR5 antagonists
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Structure-activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity.
- Hammerland, Lance G.,Johansson, Martin,Malmstroem, Jonas,Mattsson, Jan P.,Minidis, Alexander B. E.,Nilsson, Karolina,Peterson, Alecia,Wensbo, David,Wallberg, Andreas,Oesterlund, Krister
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p. 2467 - 2469
(2007/10/03)
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- NEW COMPOUNDS
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 11
(2010/02/13)
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- Preparation of Triazolopyrimidines as Potential Antiasthma Agents
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With the use of the human basophil histamine release assay, 5-aryl-2-aminotriazolopyrimidines were found to be active as mediator release inhibitors.These compounds were prepared by reacting arylamidines with sodium ethyl formylacetate or with ethyl propiolate to give pyrimidinones.Treatment with phosphorus oxychloride gave a chloropyrimidine, which was converted to a hydrazinopyrimidine with hydrazine.Cyclization, using cyanogen bromide, gave the triazolopyrimidines, after a Dimroth rearrangement.Following a structure-activity evaluation, the5--2-amino (8-10), 5-(3-bromophenyl)-2-amino (8-13), 5--2-amino (8-11), and 5-(4-pyridinyl)-2-amino (6-7) compounds were found to have the best activity.They were chosen for further pharmacological and toxicological study.
- Medwid, Jeffrey B.,Paul, Rolf,Baker, Jannie S.,Brockman, John A.,Du, Mila T.,et al.
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p. 1230 - 1241
(2007/10/02)
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