George D Hartman
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Explore the profile of George D Hartman including associated specialties, affiliations and a list of published articles.
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113
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1450
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Recent Articles
21.
Roecker A, Mercer S, Schreier J, Cox C, Fraley M, Steen J, et al.
ChemMedChem
. 2013 Dec;
9(2):311-22.
PMID: 24376006
The field of small-molecule orexin antagonist research has evolved rapidly in the last 15 years from the discovery of the orexin peptides to clinical proof-of-concept for the treatment of insomnia....
22.
Mercer S, Roecker A, Garson S, Reiss D, Harrell C, Murphy K, et al.
Bioorg Med Chem Lett
. 2013 Nov;
23(24):6620-4.
PMID: 24215892
The orexin (or hypocretin) system has been identified as a novel target for the treatment of insomnia due to the wealth of biological and genetic data discovered over the past...
23.
Kuduk S, Di Marco C, Bodmer-Narkevitch V, Cook S, Cato M, Jovanovska A, et al.
ACS Chem Neurosci
. 2012 Jul;
1(1):19-24.
PMID: 22778804
The synthesis, structure-activity relationship (SAR), and pharmacological evaluation of analogs of the acid-sensing ion channel (ASIC) inhibitor A-317567 are reported. It was found that the compound with an acetylenic linkage...
24.
Dudkin V, Rickert K, Kreatsoulas C, Wang C, Arrington K, Fraley M, et al.
Bioorg Med Chem Lett
. 2012 Mar;
22(7):2609-12.
PMID: 22374217
Pyridyl aminothiazoles comprise a novel class of ATP-competitive Chk1 inhibitors with excellent inhibitory potential. Modification of the core with ethylenediamine amides provides compounds with low picomolar potency and very high...
25.
Dudkin V, Wang C, Arrington K, Fraley M, Hartman G, Stirdivant S, et al.
Bioorg Med Chem Lett
. 2012 Feb;
22(7):2613-9.
PMID: 22365762
Translation of significant biochemical activity of pyridyl aminothiazole class of Chk1 inhibitors into functional CEA potency required analysis and adjustment of both physical properties and kinase selectivity profile of the...
26.
Coleman P, Schreier J, Cox C, Breslin M, Whitman D, Bogusky M, et al.
ChemMedChem
. 2012 Feb;
7(3):415-24, 337.
PMID: 22307992
Insomnia is a common disorder that can be comorbid with other physical and psychological illnesses. Traditional management of insomnia relies on general central nervous system (CNS) suppression using GABA modulators....
27.
Bungard C, Hartman G, Manikowski J, Perkins J, Bai C, Brandish P, et al.
Bioorg Med Chem
. 2011 Nov;
19(24):7374-86.
PMID: 22079253
A series of partial agonists of the Glucocorticoid Receptor were prepared targeting reduced transactivation activity, while maintaining significant transrepression activity. Incorporation of an ortho-aryl amide produced compounds with the desired...
28.
Kuduk S, Chang R, Di Marco C, Pitts D, Greshock T, Ma L, et al.
J Med Chem
. 2011 Jun;
54(13):4773-80.
PMID: 21682298
One approach to ameliorate the cognitive decline in Alzheimer's disease (AD) has been to restore neuronal signaling from the basal forebrain cholinergic system via the activation of the M(1) muscarinic...
29.
Kuduk S, Chang R, Di Marco C, DiPardo R, Cook S, Cato M, et al.
Bioorg Med Chem Lett
. 2011 Jun;
21(14):4255-8.
PMID: 21669528
A series of benzothiophene methyl amines were examined in an effort to identify non-amidine chemotypes with reduced polypharmacology from existing leads with the goal of finding potent ASIC3 channel blockers...
30.
Trotter B, Nanda K, Burgey C, Potteiger C, Deng J, Green A, et al.
Bioorg Med Chem Lett
. 2011 Mar;
21(8):2354-8.
PMID: 21420860
A new series of imidazopyridine CB2 agonists is described. Structural optimization improved CB2/CB1 selectivity in this series and conferred physical properties that facilitated high in vivo exposure, both centrally and...