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Michael S Wolff

Explore the profile of Michael S Wolff including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 7
Citations 47
Followers 0
Related Specialties
Biochemistry
Chemistry
Top 10 Co-Authors
Tom G Holt
M Gerard Waters
James R Tata
Steven L Colletti
Subharekha Raghavan
Ester Carballo-Jane
Hong C Shen
Milton L Hammond
Ning Ren
Fa-Xiang Ding
Published In
Bioorg Med Chem Lett
J Med Chem
Affiliations
Soon will be listed here.
Recent Articles
1.
The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties
Imbriglio J, DiRocco D, Bodner R, Raghavan S, Chen W, Marley D, et al.
Bioorg Med Chem Lett . 2010 Dec; 21(9):2721-4. PMID: 21185185
Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties.
2.
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a
Imbriglio J, Chang S, Liang R, Raghavan S, Schmidt D, Smenton A, et al.
Bioorg Med Chem Lett . 2010 Jul; 20(15):4472-4. PMID: 20615702
5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic...
3.
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate
Shen H, Ding F, Raghavan S, Deng Q, Luell S, Forrest M, et al.
J Med Chem . 2010 Feb; 53(6):2666-70. PMID: 20184326
Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR109A) agonists. Compound 1e (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good...
4.
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats
Shen H, Ding F, Deng Q, Wilsie L, Krsmanovic M, Taggart A, et al.
J Med Chem . 2009 Mar; 52(8):2587-602. PMID: 19309152
Tricyclic analogues were rationally designed as the high affinity niacin receptor G-protein-coupled receptor 109A (GPR109A) agonists by overlapping three lead structures. Various tricyclic anthranilide and cycloalkene carboxylic acid full agonists...
5.
Discovery of imidazole carboxamides as potent and selective CCK1R agonists
Zhu C, Hansen A, Bateman T, Chen Z, Holt T, Hubert J, et al.
Bioorg Med Chem Lett . 2008 Jul; 18(15):4393-6. PMID: 18614364
High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl...
6.
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists
Raghavan S, Tria G, Shen H, Ding F, Taggart A, Ren N, et al.
Bioorg Med Chem Lett . 2008 May; 18(11):3163-7. PMID: 18477506
The design, synthesis, and biological activity of a series of cycloalkene acid-based niacin receptor agonists are described. This led to the discovery that tetrahydro anthranilic acid is an excellent surrogate...
7.
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor
Shen H, Ding F, Luell S, Forrest M, Carballo-Jane E, Wu K, et al.
J Med Chem . 2007 Nov; 50(25):6303-6. PMID: 17994679
Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and...