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Page 1
Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.
Garbaccio RM, Brnardic EJ, Fraley ME, Hartman GD, Hutson PH, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Small JH, Tang C, Kuo Y, Jacobson MA. Garbaccio RM, et al. Among authors: hartman gd. ACS Med Chem Lett. 2010 Jul 12;1(8):406-10. doi: 10.1021/ml100115a. eCollection 2010 Nov 11. ACS Med Chem Lett. 2010. PMID: 24900224 Free PMC article.
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, Sur SM, Hartman GD. Brnardic EJ, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31. Bioorg Med Chem Lett. 2010. PMID: 20409708
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Lindsley CW, et al. Among authors: hartman gd. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW. Zhao Z, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. doi: 10.1016/j.bmcl.2006.11.081. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17210250
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Brnardic EJ, Garbaccio RM, Fraley ME, Tasber ES, Steen JT, Arrington KL, Dudkin VY, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C. Brnardic EJ, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5989-94. doi: 10.1016/j.bmcl.2007.07.051. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17804227
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Converso A, Hartingh T, Garbaccio RM, Tasber E, Rickert K, Fraley ME, Yan Y, Kreatsoulas C, Stirdivant S, Drakas B, Walsh ES, Hamilton K, Buser CA, Mao X, Abrams MT, Beck SC, Tao W, Lobell R, Sepp-Lorenzino L, Zugay-Murphy J, Sardana V, Munshi SK, Jezequel-Sur SM, Zuck PD, Hartman GD. Converso A, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1240-4. doi: 10.1016/j.bmcl.2008.12.076. Epub 2008 Dec 24. Bioorg Med Chem Lett. 2009. PMID: 19155174
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Converso A, Hartingh T, Fraley ME, Garbaccio RM, Hartman GD, Huang SY, Majercak JM, McCampbell A, Na SJ, Ray WJ, Savage MJ, Wolffe C, Yeh S, Yu Y, White R, Zhang R. Converso A, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2737-40. doi: 10.1016/j.bmcl.2014.04.034. Epub 2014 Apr 18. Bioorg Med Chem Lett. 2014. PMID: 24813734
Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.
Barrow JC, Rittle KE, Reger TS, Yang ZQ, Bondiskey P, McGaughey GB, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Marino MJ, Kuzmick Graufelds V, Uebele VN, Renger JJ. Barrow JC, et al. Among authors: hartman gd. ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900180 Free PMC article.
Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.
Yang ZQ, Schlegel KA, Shu Y, Reger TS, Cube R, Mattern C, Coleman PJ, Small J, Hartman GD, Ballard J, Tang C, Kuo Y, Prueksaritanont T, Nuss CE, Doran S, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Taylor AB, Zeng W, Fang W, Chavez-Eng C, Troyer MD, Luk JA, Laethem T, Cook WO, Renger JJ, Barrow JC. Yang ZQ, et al. Among authors: hartman gd. ACS Med Chem Lett. 2010 Aug 24;1(9):504-9. doi: 10.1021/ml100170e. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900239 Free PMC article.
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Fraley ME, Steen JT, Brnardic EJ, Arrington KL, Spencer KL, Hanney BA, Kim Y, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C. Fraley ME, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6049-53. doi: 10.1016/j.bmcl.2006.08.118. Epub 2006 Sep 15. Bioorg Med Chem Lett. 2006. PMID: 16978863
171 results