Michael B Tollefson
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Explore the profile of Michael B Tollefson including associated specialties, affiliations and a list of published articles.
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8
Citations
58
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Recent Articles
1.
Tollefson M, Acker B, Jacobsen E, Hughes R, Walker J, Fox D, et al.
Bioorg Med Chem Lett
. 2010 May;
20(10):3120-4.
PMID: 20443228
1H-Pyrazolo[4,3-d]pyrimidines are a class of potent and selective second generation phosphodiesterase 5 (PDE5) inhibitors. This work explores the potency, selectivity and efficacy of 1-(2-ethoxyethyl)-1H-pyrazolo[4,5-d]pyrimidines as PDE5 inhibitors resulting in the...
2.
Tollefson M, Acker B, Jacobsen E, Hughes R, Walker J, Fox D, et al.
Bioorg Med Chem Lett
. 2010 Apr;
20(10):3125-8.
PMID: 20400309
1H-Pyrazolo[4,3-d]pyrimidines were previously disclosed as a potent second generation class of phosphodiesterase 5 (PDE5) inhibitors. This work explores the advancement of more selective and potent PDE5 inhibitors resulting from the...
3.
Owen D, Walker J, Jacobsen E, Freskos J, Hughes R, Brown D, et al.
Bioorg Med Chem Lett
. 2009 Jun;
19(15):4088-91.
PMID: 19540112
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl,...
4.
Boys M, Schretzman L, Chandrakumar N, Tollefson M, Mohler S, Downs V, et al.
Bioorg Med Chem Lett
. 2005 Nov;
16(4):839-44.
PMID: 16298127
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the...
5.
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 2)
Huang H, Tremont S, Lee L, Keller B, Carpenter A, Wang C, et al.
J Med Chem
. 2005 Sep;
48(18):5853-68.
PMID: 16134951
In the preceding paper several compounds were reported as potent apical sodium-codependent bile acid transporter (ASBT) inhibitors. Since the primary site for active bile acid reabsorption is via ASBT, which...
6.
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 1)
Tremont S, Lee L, Huang H, Keller B, Banerjee S, Both S, et al.
J Med Chem
. 2005 Sep;
48(18):5837-52.
PMID: 16134950
Elevated plasma levels of low-density lipoprotein (LDL) cholesterol are a major risk factor for atherosclerosis leading to coronary artery disease (CAD), which remains the main cause of mortality in Western...
7.
Tollefson M, Kolodziej S, Fletcher T, Vernier W, Beaudry J, Keller B, et al.
Bioorg Med Chem Lett
. 2003 Oct;
13(21):3727-30.
PMID: 14552767
A series of 5-aryl-3,3-dibutyl-7-(dimethylamino)-1,2-benzothiazepin-4-ol 1,1-dioxides were prepared and were found to inhibit the apical sodium co-dependent bile acid transporter (ASBT) for the potential treatment for hyperlipidemia. Several 1,2-benzothiazepines exhibited low...
8.
Reinhard E, Wang J, Durley R, Fobian Y, Grapperhaus M, Hickory B, et al.
J Med Chem
. 2003 May;
46(11):2152-68.
PMID: 12747787
A novel series of substituted N-[3-(1,1,2,2-tetrafluoroethoxy)benzyl]-N-(3-phenoxyphenyl)-trifluoro-3-amino-2-propanols is described which potently and reversibly inhibit cholesteryl ester transfer protein (CETP). Starting from the initial lead 1, various substituents were introduced into the...