George Doss
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Explore the profile of George Doss including associated specialties, affiliations and a list of published articles.
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7
Citations
65
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Recent Articles
1.
Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe J, et al.
Bioorg Med Chem Lett
. 2015 Nov;
25(24):5767-71.
PMID: 26546218
A series of novel substituted-[(3R)-amino-2-(2,5-difluorophenyl)]tetrahydro-2H-pyran analogs have been prepared and evaluated as potent, selective and orally active DPP-4 inhibitors. These efforts lead to the discovery of a long acting DPP-4...
2.
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe J, et al.
J Med Chem
. 2014 Mar;
57(8):3205-12.
PMID: 24660890
In our effort to discover DPP-4 inhibitors with added benefits over currently commercially available DPP-4 inhibitors, MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor...
3.
Tan E, Hartmann G, Chen Q, Pereira A, Bradley S, Doss G, et al.
Drug Metab Dispos
. 2009 Dec;
38(3):459-73.
PMID: 20016052
The pharmacokinetics and metabolism of anacetrapib (MK-0859), a novel cholesteryl ester transfer protein inhibitor, were examined in rats and rhesus monkeys. Anacetrapib exhibited a low clearance in both species and...
4.
Morriello G, DeVita R, Mills S, Young J, Lin P, Doss G, et al.
Bioorg Med Chem
. 2008 Feb;
16(5):2156-70.
PMID: 18248994
Previous work on human NK(1) antagonists in which the core of the structure is a substituted pyrrolidine has been disclosed. These compounds showed good binding affinity and functional IP activity,...
5.
Karanam B, Madeira M, Bradley S, Wenning L, Desai R, Soli E, et al.
Drug Metab Dispos
. 2007 Apr;
35(7):1196-202.
PMID: 17431030
[(3R)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopentaindol-3-yl]acetic acid (MK-0524) is a potent orally active human prostaglandin D(2) receptor 1 antagonist that is currently under development for the prevention of niacin-induced flushing. The metabolism and excretion of...
6.
Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes
Xu S, Zhu B, Teffera Y, Pan D, Caldwell C, Doss G, et al.
Drug Metab Dispos
. 2004 Oct;
33(1):121-30.
PMID: 15486074
The current study evaluated the potential for two dipeptidyl peptidase-IV (DPP-IV) inhibitor analogs (1S)-1-(trans-4-([(4-trifluoromethoxyphenyl)sulfonyl]amino)cyclohexyl)-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethanaminium chloride and (1S)-1-(trans-4-([(2,4-difluorophenyl)sulfonyl]amino)cyclohexyl)-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethanaminium chloride (MRL-A and MRL-B), containing a fluoropyrrolidine moiety in the structure, to undergo...
7.
Lynch C, Gentry A, Hale J, Mills S, MacCoss M, Malkowitz L, et al.
Bioorg Med Chem Lett
. 2002 Feb;
12(4):677-9.
PMID: 11844699
A series of CCR5 antagonists containing bicyclic isoxazolidines was generated through a nitrone mediated cycloaddition with olefins bearing the preferred pharmacophores previously described. Potent antagonists (3 and 16) were generated...