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
31.
Manley P, Zartman A, Paone D, Burgey C, Henze D, Della Penna K, et al.
Bioorg Med Chem Lett
. 2011 Mar;
21(8):2359-64.
PMID: 21420857
A novel series of decahydroquinoline CB2 agonists is described. Optimization of the amide substituent led to improvements in CB2/CB1 selectivity as well as physical properties. Two key compounds were examined...
32.
Wolkenberg S, Zhao Z, Thut C, Maxwell J, Mcdonald T, Kinose F, et al.
J Med Chem
. 2011 Mar;
54(7):2351-8.
PMID: 21395312
Agonists of somatostatin receptor subtype 2 (sst(2)) have been proposed as therapeutics for the treatment of proliferative diabetic retinopathy and exudative age-related macular degeneration. An HTS screen identified 2-quinolones as...
33.
Kuduk S, Chang R, Di Marco C, Ray W, Ma L, Wittmann M, et al.
Bioorg Med Chem Lett
. 2011 Feb;
21(6):1710-5.
PMID: 21324684
SAR study of the piperidine moiety in a series of quinolizidinone carboxylic acid M(1) positive allosteric modulators was examined. While the SAR was generally flat, compounds were identified with high...
34.
Reger T, Yang Z, Schlegel K, Shu Y, Mattern C, Cube R, et al.
Bioorg Med Chem Lett
. 2011 Feb;
21(6):1692-6.
PMID: 21316226
A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of...
35.
Wolkenberg S, Zhao Z, Mulhearn J, Harrison S, Sanders J, Cato M, et al.
Bioorg Med Chem Lett
. 2011 Jan;
21(9):2646-9.
PMID: 21257308
The Merck Fragment Library was screened versus acid-sensing ion channel 3 (ASIC3), a novel target for the treatment of pain. Fragment hits were optimized using two strategies, and potency was...
36.
Kuduk S, Di Marco C, Cofre V, Ray W, Ma L, Wittmann M, et al.
Bioorg Med Chem Lett
. 2010 Nov;
21(9):2769-72.
PMID: 21055928
Fused aromatics such as naphthalene were identified as highly potent and CNS penetrant M(1) positive allosteric modulators during an SAR study to replace the phenyl B-ring linkage.
37.
Schlegel K, Yang Z, Reger T, Shu Y, Cube R, Rittle K, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(17):5147-52.
PMID: 20673719
The discovery and synthesis of 4,4-disubstituted quinazolinones as T-type calcium channel antagonists is reported. Based on lead compounds 2 and 3, a focused SAR campaign driven by the optimization of...
38.
Trotter B, Nanda K, Manley P, Uebele V, Condra C, Gotter A, et al.
Bioorg Med Chem Lett
. 2010 Jul;
20(15):4704-8.
PMID: 20615693
A new structural class of potent antagonists of the Neuropeptide S Receptor (NPSR) is reported. High-throughput screening identified a tricyclic imidazole antagonist of NPSR, and medicinal chemistry optimization of this...
39.
Coleman P, Schreier J, Roecker A, Mercer S, McGaughey G, Cox C, et al.
Bioorg Med Chem Lett
. 2010 Jul;
20(14):4201-5.
PMID: 20610153
Orexins are excitatory neuropeptides that regulate arousal and sleep. Orexin receptor antagonists promote sleep and offer potential as a new therapy for the treatment of insomnia. In this Letter, we...
40.
Cox C, Breslin M, Whitman D, Schreier J, McGaughey G, Bogusky M, et al.
J Med Chem
. 2010 Jun;
53(14):5320-32.
PMID: 20565075
Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified in recent years. One notable exception...