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Page 1
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA, Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE. Deskus JA, et al. Among authors: molski tf. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23010264
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.
Deskus JA, Epperson JR, Sloan CP, Cipollina JA, Dextraze P, Qian-Cutrone J, Gao Q, Ma B, Beno BR, Mattson GK, Molski TF, Krause RG, Taber MT, Lodge NJ, Mattson RJ. Deskus JA, et al. Among authors: molski tf. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3099-104. doi: 10.1016/j.bmcl.2007.03.040. Epub 2007 Mar 16. Bioorg Med Chem Lett. 2007. PMID: 17391962
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.
Dalton King H, Denhart DJ, Deskus JA, Ditta JL, Epperson JR, Higgins MA, Kung JE, Marcin LR, Sloan CP, Mattson GK, Molski TF, Krause RG, Bertekap RL Jr, Lodge NJ, Mattson RJ, Macor JE. Dalton King H, et al. Among authors: molski tf. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5647-51. doi: 10.1016/j.bmcl.2007.07.083. Epub 2007 Aug 22. Bioorg Med Chem Lett. 2007. PMID: 17766113
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE. Hartz RA, et al. Among authors: molski tf. J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. J Med Chem. 2009. PMID: 19552436
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE. Hartz RA, et al. Among authors: molski tf. J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y. J Med Chem. 2009. PMID: 19552437
Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Denhart DJ, Deskus JA, Ditta JL, Gao Q, Dalton King H, Kozlowski ES, Meng Z, LaPaglia MA, Mattson GK, Molski TF, Taber MT, Lodge NJ, Mattson RJ, Macor JE. Denhart DJ, et al. Among authors: molski tf. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4031-3. doi: 10.1016/j.bmcl.2009.06.026. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19560923
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ. Hartz RA, et al. Among authors: molski tf. J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v. J Med Chem. 2009. PMID: 19954247
98 results